JP7461876B2 - Devil's claw extract, various compositions containing same and method for producing devil's claw extract - Google Patents
Devil's claw extract, various compositions containing same and method for producing devil's claw extract Download PDFInfo
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- JP7461876B2 JP7461876B2 JP2020521782A JP2020521782A JP7461876B2 JP 7461876 B2 JP7461876 B2 JP 7461876B2 JP 2020521782 A JP2020521782 A JP 2020521782A JP 2020521782 A JP2020521782 A JP 2020521782A JP 7461876 B2 JP7461876 B2 JP 7461876B2
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- MECHNRXZTMCUDQ-RKHKHRCZSA-N vitamin D2 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)/C=C/[C@H](C)C(C)C)=C\C=C1\C[C@@H](O)CCC1=C MECHNRXZTMCUDQ-RKHKHRCZSA-N 0.000 description 1
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- 239000002446 δ-tocopherol Substances 0.000 description 1
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- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
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Description
本発明は、デビルズクロー抽出物、それを含有する各種組成物及びデビルズクロー抽出物の製造方法に関する。また、本発明は、外用組成物、内服用組成物、食品組成物に関する。The present invention relates to a devil's claw extract, various compositions containing the same, and a method for producing the devil's claw extract. The present invention also relates to a composition for external use, a composition for internal use, and a food composition.
いつの時代も人々の健康、美容への関心は尽きない。近年特に、美白、抗シワ、アンチエイジング効果のある化粧品、機能性食品、サプリメント等が注目されている。また、大気汚染物質には、PM2.5や黄砂、排気ガス、ハウスダストなど様々な微小粒子物質があり、眼、呼吸器、心臓などの循環器への影響については以前よりよく知られている。さらにこれら部位での疾患に加えて、大気汚染物質により、アトピーやアレルギー、バリア機能の低下等の皮膚疾患(皮膚障害)を引き起こすことも知られるようになった。そのため、抗炎症、肌あれ改善等の効果のある化粧品、機能性食品、サプリメント等も注目されている。このような中、美白、抗シワ、アンチエイジング、抗炎症、肌あれ改善等に対してより優れた効果を奏する新規の素材が常に求められている。People are always interested in health and beauty. In recent years, cosmetics, functional foods, supplements, etc. with whitening, anti-wrinkle, and anti-aging effects have been attracting attention. In addition, air pollutants include various fine particulate matter such as PM2.5, yellow sand, exhaust gas, and house dust, and their effects on the eyes, respiratory system, heart, and other circulatory systems have long been known. In addition to diseases in these areas, it has also become known that air pollutants can cause skin diseases (skin disorders) such as atopy, allergies, and impaired barrier function. For this reason, cosmetics, functional foods, supplements, etc. with anti-inflammation and skin roughness improvement effects have also been attracting attention. In this situation, new materials that have better effects on whitening, anti-wrinkle, anti-aging, anti-inflammation, and skin roughness improvement are constantly in demand.
一方、デビルズクロー(Harpagophytum procumbens)は南アフリカ原産のゴマ科の多年草植物で、硬いトゲのある実ができることからデビルズクローと呼ばれ、薬用植物として古くから利用されている。その作用としては、抗炎症作用、抗菌作用、消炎鎮痛作用等が知られており、伝統的に解熱鎮痛、消化不良の治療に使用されてきた。また、変形性膝関節症、リウマチ等の免疫性疾患の予防及び症状改善に有効であることも知られている(非特許文献1及び2、並びに特許文献1及び2参照)。さらに、デビルズクロー抽出物には肌荒れ改善効果、肌のはり、シワ改善効果が認められ、その作用を利用した皮膚外用剤が開示されている(特許文献3参照)。その有効成分としては、ハルパゴシド等のイリドイド類の存在が明らかとなっている。これら有効成分には各種薬理作用があり、抗炎症作用に拮抗する成分も含まれていたり、また投与経路、適用部位、適用対象によっては使用が制限されるなどの不利な状況になることもある(特許文献4及び5並びに非特許文献3参照)。さらにこれら成分は苦味剤としても知られている(特許文献6参照)。On the other hand, Devil's Claw (Harpagophytum procumbens) is a perennial plant of the Pedaliaceae family native to South Africa. It is called Devil's Claw because it produces hard, thorny fruits, and has been used as a medicinal plant for a long time. Its effects include anti-inflammatory, antibacterial, and anti-inflammatory analgesic effects, and it has traditionally been used to treat fever, analgesia, and indigestion. It is also known to be effective in preventing and improving immune diseases such as osteoarthritis of the knee and rheumatism (see Non-Patent
大気エアロゾル粒子に起因する皮膚炎症の抑制剤としては、グミ科ヒッポファエ属の抽出物を有効成分とする製剤が知られている(特許文献7参照)。また、大気汚染物質等からの保護を目的とした、所定量のメタケイ酸アルミン酸マグネシウムと、オクチルメトキシシンナメート及び/又はジエチルアミノヒドロキシベンゾイル安息香酸ヘキシルとを含有するスキンケア化粧料(特許文献8参照)、ヒアルロン酸および/またはその塩を有効成分として含有する、アンチポリューション剤(特許文献9参照)が知られている。As an inhibitor of skin inflammation caused by atmospheric aerosol particles, a preparation containing an extract of the Hippophae genus of the Elaeagnaceae family as an active ingredient is known (see Patent Document 7). In addition, a skin care cosmetic containing a specified amount of magnesium aluminometasilicate, octyl methoxycinnamate and/or diethylaminohydroxybenzoyl hexyl benzoate for the purpose of protection from air pollutants and the like (see Patent Document 8), and an anti-pollution agent containing hyaluronic acid and/or a salt thereof as an active ingredient (see Patent Document 9) are also known.
本発明は、かかる状況下においてなされたものであり、健康、美容、特に美白、抗シワ、アンチエイジング、抗炎症、肌あれ改善等に優れた効果を奏する、新規の素材を提供すること、またそのような素材の製造方法を提供することを課題とする。The present invention was made under such circumstances, and its objective is to provide a new material that has excellent effects on health and beauty, particularly in terms of whitening, anti-wrinkle, anti-aging, anti-inflammation, and improving rough skin, as well as to provide a method for producing such a material.
本発明者らは、美白、抗シワ、アンチエイジング等の美容効果や、関節症の緩和・改善、健康増進効果、抗炎症、肌あれ改善効果等を奏する、新しい素材を探求する中で、デビルズクロー抽出物の有効成分の1種であるハルパゴシドを除去した後の残渣の各種作用を検討したところ、予想外の種々の有効性を確認することができ、新たな素材として活用できることを見出し、本発明を完成するに至った。 In the course of searching for new materials that have cosmetic effects such as whitening, anti-wrinkle and anti-aging, as well as effects such as the alleviation and improvement of arthritis, health promotion, anti-inflammatory properties and skin-improvement effects, the inventors investigated the various effects of the residue left after removing harpagoside, one of the active ingredients in devil's claw extract. They were able to confirm a variety of unexpected benefits and discovered that the residue could be used as a new material, which led to the completion of the present invention.
即ち、本発明の要旨は以下の通りである。In other words, the gist of the present invention is as follows.
[1]ハルパゴシド含有量が1.0重量%以下である、デビルズクロー抽出物。
[2]スタキオースの含有量(重量%)に対するハルパゴシドの含有量(重量%)が、0~1.0である、[1]に記載のデビルズクロー抽出物。
[3]デビルズクロー抽出物が乾燥粉末である場合、又はデビルズクロー抽出物が液体である場合にはそれを乾燥粉末とした場合、その0.5重量%濃度の水溶液の、可視光領域の波長における吸光度が0.1以下となることを特徴とする、[1]又は[2]に記載のデビルズクロー抽出物。
[4][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、メラニン合成酵素遺伝子発現抑制用組成物。
[5][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、美白用組成物。
[6][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、コラーゲン産生促進用組成物。
[7][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、エラスチン線維形成促進用組成物。
[8][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、ヒアルロン酸産生促進用組成物。
[9][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、皮膚のバリア機能亢進用組成物。
[10][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、アンチポリューション組成物。
[11][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、大気汚染物質誘発炎症用の抗炎症組成物。
[12][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、大気汚染物質による皮膚障害改善用組成物。
[13][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、Gobi Kosa Dust誘発炎症用の抗炎症組成物。
[14][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、関節症の緩和・改善用組成物。
[15][1]~[3]のいずれかに記載のデビルズクロー抽出物を含有する、炎症性物質発現抑制用組成物。
[16]炎症性物質が、IL-1β、IL-6又はIL-8である、[15]に記載の組成物。
[17][1]~[3]のいずれかに記載のデビルズクロー抽出物、又は[4]~[16]のいずれかに記載の組成物を含有する、外用組成物。
[18][1]~[3]のいずれかに記載のデビルズクロー抽出物、又は[4]~[13]、[15]、[16]のいずれかに記載の組成物を含有する、化粧料組成物。
[19][1]~[3]のいずれかに記載のデビルズクロー抽出物、又は[4]~[16]のいずれかに記載の組成物を含有する、経口用組成物。
[20][1]~[3]のいずれかに記載のデビルズクロー抽出物、又は[4]~[16]のいずれかに記載の組成物を含有する、食品組成物。
[21][1]~[3]のいずれかに記載のデビルズクロー抽出物、又は[6]~[8]、[10]、[11]、[13]、[15]、[16]のいずれかに記載の組成物を含有する、眼科用組成物。
[22](A)デビルズクロー乾燥粉末の抽出液を得る工程、及び
(B)上記抽出液を、疎水性成分を吸着させる樹脂で処理して精製抽出液を得る工程
を含む、デビルズクロー抽出物の製造方法。
[23](A)デビルズクロー乾燥粉末の抽出液を得る工程、及び
(B)上記抽出液を、疎水性成分を吸着させる樹脂で処理して精製抽出液を得る工程
を含む製造方法により製造される、[1]~[3]のいずれかに記載のデビルズクロー抽出物。
[1] Devil's claw extract having a harpagoside content of 1.0% by weight or less.
[2] The devil's claw extract according to [1], wherein the ratio of the harpagoside content (wt%) to the stachyose content (wt%) is 0 to 1.0.
[3] The devil's claw extract according to [1] or [2], characterized in that when the devil's claw extract is a dry powder, or when the devil's claw extract is a liquid and is made into a dry powder, the absorbance of a 0.5 wt% aqueous solution of the devil's claw extract in the visible light region is 0.1 or less at wavelengths.
[4] A composition for inhibiting melanin synthesis enzyme gene expression, comprising the devil's claw extract according to any one of [1] to [3].
[5] A whitening composition comprising the devil's claw extract according to any one of [1] to [3].
[6] A composition for promoting collagen production, comprising the devil's claw extract according to any one of [1] to [3].
[7] A composition for promoting elastin fiber formation, comprising the devil's claw extract according to any one of [1] to [3].
[8] A composition for promoting hyaluronic acid production, comprising the devil's claw extract according to any one of [1] to [3].
[9] A composition for enhancing the skin barrier function, comprising the devil's claw extract according to any one of [1] to [3].
[10] An anti-pollution composition comprising the devil's claw extract according to any one of [1] to [3].
[11] An anti-inflammatory composition for air pollutant-induced inflammation, comprising the devil's claw extract according to any one of [1] to [3].
[12] A composition for improving skin disorders caused by air pollutants, comprising the devil's claw extract according to any one of [1] to [3].
[13] An anti-inflammatory composition for Gobi Kosa Dust-induced inflammation, comprising the devil's claw extract according to any one of [1] to [3].
[14] A composition for alleviating or improving arthropathy, comprising the devil's claw extract according to any one of [1] to [3].
[15] A composition for suppressing the expression of inflammatory substances, comprising the devil's claw extract according to any one of [1] to [3].
[16] The composition described in [15], wherein the inflammatory substance is IL-1β, IL-6 or IL-8.
[17] A composition for external use comprising the devil's claw extract according to any one of [1] to [3], or the composition according to any one of [4] to [16].
[18] A cosmetic composition comprising the devil's claw extract according to any one of [1] to [3], or the composition according to any one of [4] to [13], [15], or [16].
[19] A composition for oral administration, comprising the devil's claw extract according to any one of [1] to [3], or the composition according to any one of [4] to [16].
[20] A food composition comprising the devil's claw extract according to any one of [1] to [3], or the composition according to any one of [4] to [16].
[21] An ophthalmic composition comprising the devil's claw extract according to any one of [1] to [3], or the composition according to any one of [6] to [8], [10], [11], [13], [15], or [16].
[22] A method for producing a devil's claw extract, comprising: (A) obtaining an extract from a dry powder of devil's claw; and (B) treating the extract with a resin that adsorbs hydrophobic components to obtain a purified extract.
[23] The devil's claw extract according to any one of [1] to [3], which is produced by a production method including: (A) obtaining an extract from a dry powder of devil's claw; and (B) treating the extract with a resin that adsorbs hydrophobic components to obtain a purified extract.
本発明のデビルズクロー抽出物は、従来のデビルズクロー抽出物から、有効成分として知られていたハルパゴシド等の疎水性の物質を除去したものであり、ハルパゴシドの含有量が1.0重量%以下と顕著に抑えられた新規のエキスである。従来のデビルズクロー抽出物と異なり、独特の着色や臭い、苦味が生じないことから安定性にも優れ、溶解性も高いことから、様々な製品に配合し易いという利点がある。また、投与経路、適用部位、適用対象による不都合な事象の発現が抑制されることも期待できる。さらに、この本発明のデビルズクロー抽出物は、皮膚におけるメラニン合成酵素遺伝子発現抑制作用、コラーゲン産生促進作用、エラスチン線維形成促進作用、ヒアルロン酸産生促進作用、大気汚染物質により誘発される炎症性物質の産生抑制効果、大気汚染物質により誘発される皮膚障害(バリア機能低下を含む)を改善する効果等を有し、美白、抗シワ、アンチエイジング、関節症の緩和・改善効果、抗炎症効果(アンチポリューション)、皮膚のバリア機能亢進効果も期待できる。以上のことから、本発明のデビルズクロー抽出物は、化粧品、医薬品、医薬部外品、食品(機能性食品、サプリメント、ドリンク剤等)等として、その形態については外用組成物、経口用組成物、眼科用組成物等として好適に使用することができる。The devil's claw extract of the present invention is a novel extract obtained by removing hydrophobic substances such as harpagoside, which was known as an active ingredient, from conventional devil's claw extracts, and is a novel extract in which the content of harpagoside is significantly suppressed to 1.0% by weight or less. Unlike conventional devil's claw extracts, it has excellent stability and high solubility because it does not produce unique coloring, odor, or bitterness, and therefore has the advantage of being easily blended into various products. It is also expected that the occurrence of undesirable events due to the administration route, application site, or application subject can be suppressed. Furthermore, the devil's claw extract of the present invention has an effect of suppressing melanin synthesis enzyme gene expression in the skin, an effect of promoting collagen production, an effect of promoting elastin fiber formation, an effect of promoting hyaluronic acid production, an effect of suppressing the production of inflammatory substances induced by air pollutants, an effect of improving skin disorders (including reduced barrier function) induced by air pollutants, etc., and can also be expected to have whitening, anti-wrinkle, anti-aging, arthritis relief/improvement effects, anti-inflammatory effects (anti-pollution), and an effect of enhancing the barrier function of the skin. From the above, the devil's claw extract of the present invention can be suitably used as cosmetics, medicines, quasi-drugs, foods (functional foods, supplements, drinks, etc.), and in the form of external compositions, oral compositions, ophthalmic compositions, etc.
以下、本発明について詳細に説明する。なお、本明細書中で使用される用語は、特に言及しない限り、当該技術分野で通常用いられる意味で解釈される。The present invention will now be described in detail. In addition, the terms used in this specification shall be interpreted as having the meanings normally used in the relevant technical field unless otherwise specified.
[デビルズクロー抽出物]
本発明のデビルズクロー抽出物は、従来のデビルズクロー抽出物から、有効成分として知られていたハルパゴシド等の疎水性の物質を、樹脂等を用いて除去したものであり、ハルパゴシドの含有量が1.0重量%以下であることを特徴とする新規のエキスである。
[Devil's Claw Extract]
The devil's claw extract of the present invention is a novel extract obtained by removing hydrophobic substances such as harpagoside, which are known to be active ingredients, from conventional devil's claw extracts using resins or the like, and is characterized by having a harpagoside content of 1.0% by weight or less.
デビルズクロー(Harpagophytum procumbens)は南アフリカ原産のゴマ科の多年草植物で、その塊茎部分は薬用植物として古くから利用されている。このデビルズクローには、抗炎症作用や鎮痛作用があることが知られているイリドイド配糖体であるハルパゴシドが多く含まれている。また、ポリフェノール類、桂皮酸、多糖類等の様々な成分が含まれていることが知られている。Devil's claw (Harpagophytum procumbens) is a perennial plant of the Pedaliaceae family native to South Africa, and its tubers have long been used as a medicinal plant. Devil's claw contains a large amount of harpagoside, an iridoid glycoside known to have anti-inflammatory and analgesic effects. It is also known to contain various components such as polyphenols, cinnamic acid, and polysaccharides.
(内容成分)
本発明のデビルズクロー抽出物は上述のとおり、樹脂等を用いて疎水性の物質を除去して得られるものであるため、ハルパゴシドの含有量が1.0重量%以下である。本発明のデビルズクロー抽出物においては、その安定性、着色の度合い、臭いの観点から、ハルパゴシドの含有量は少ない方が好ましく、0.5重量%以下であることが好ましく、0.3重量%以下であることがより好ましく、0.1重量%以下であることがさらに好ましく、0.05重量%以下であることが特に好ましい。即ち、本発明のデビルズクロー抽出物におけるハルパゴシドの含有量は、0~1.0重量%であり、0~0.5重量%であることが好ましく、0~0.3重量%であることがより好ましく、0~0.1重量%であることがさらに好ましく、0~0.05重量%であることが特に好ましい。なお、ハルパゴシドの含有量は、HPLCを使用した分析により定量することができる。
(Ingredients)
As described above, the devil's claw extract of the present invention is obtained by removing hydrophobic substances using a resin or the like, and therefore the content of harpagoside is 1.0% by weight or less. In the devil's claw extract of the present invention, from the viewpoints of stability, degree of coloration, and odor, the content of harpagoside is preferably low, and is preferably 0.5% by weight or less, more preferably 0.3% by weight or less, even more preferably 0.1% by weight or less, and particularly preferably 0.05% by weight or less. That is, the content of harpagoside in the devil's claw extract of the present invention is 0 to 1.0% by weight, preferably 0 to 0.5% by weight, more preferably 0 to 0.3% by weight, even more preferably 0 to 0.1% by weight, and particularly preferably 0 to 0.05% by weight. The content of harpagoside can be quantified by analysis using HPLC.
本発明のデビルズクロー抽出物はハルパゴシド以外の成分として、ハルパギド、スタキオース、スクロース、ラフィノース等の多糖類、アントシアニン等のポリフェノール類、桂皮酸等を含んでいてもよい。本発明のデビルズクロー抽出物は、樹脂等により疎水性の成分を吸着させて除去しているので、従来のデビルズクロー抽出物と比較して、上記ポリフェノール類の含有量は少ない傾向にある。本発明のデビルズクロー抽出物におけるポリフェノールの含有量は、2重量%以下であり、1.8重量%以下であることが好ましく、1.5重量%以下であることがより好ましく、1.0重量%以下であることがさらに好ましい。即ち、本発明のデビルズクロー抽出物におけるポリフェノールの含有量は、0~2.0重量%であり、0~1.8重量%であることが好ましく、0~1.5重量%であることがより好ましく、0~1.0重量%であることがさらに好ましい。なお、ポリフェノールの含有量は、分光光度計を使用した分析により定量することができる。The devil's claw extract of the present invention may contain polysaccharides such as harpagide, stachyose, sucrose, and raffinose, polyphenols such as anthocyanin, and cinnamic acid as components other than harpagoside. The devil's claw extract of the present invention has hydrophobic components adsorbed and removed by resins, etc., so the content of the polyphenols tends to be lower than that of conventional devil's claw extracts. The polyphenol content in the devil's claw extract of the present invention is 2% by weight or less, preferably 1.8% by weight or less, more preferably 1.5% by weight or less, and even more preferably 1.0% by weight or less. That is, the polyphenol content in the devil's claw extract of the present invention is 0 to 2.0% by weight, preferably 0 to 1.8% by weight, more preferably 0 to 1.5% by weight, and even more preferably 0 to 1.0% by weight. The polyphenol content can be quantified by analysis using a spectrophotometer.
本発明のデビルズクロー抽出物における上記スタキオースの含有量としては、50重量%以上であり、55重量%以上あることが好ましく、60重量%以上であることがより好ましく、65重量%~以上であることがさらに好ましい。The content of the above-mentioned stachyose in the devil's claw extract of the present invention is 50% by weight or more, preferably 55% by weight or more, more preferably 60% by weight or more, and even more preferably 65% by weight or more.
本発明のデビルズクロー抽出物におけるスタキオースの含有量(重量%)に対するハルパゴシドの含有量(重量%)の比、即ち、ハルパゴシドの含有量(重量%)/スタキオースの含有量(重量%)の値は、0~0.02であり、0~0.01であることが好ましく、0~0.005であることがより好ましく、0~0.003であることがさらに好ましく、0~0.001であることが特に好ましい。スタキオースの含有量(重量%)に対するハルパゴシドの含有量(重量%)の比が上記範囲内であると、本発明のデビルズクロー抽出物は、着色や臭いが生じ難いことから安定性にも優れ、溶解性も高くなることから、様々な製品に配合し易くなる。The ratio of the harpagoside content (wt%) to the stachyose content (wt%) in the devil's claw extract of the present invention, i.e., the value of the harpagoside content (wt%)/stachyose content (wt%), is 0 to 0.02, preferably 0 to 0.01, more preferably 0 to 0.005, even more preferably 0 to 0.003, and particularly preferably 0 to 0.001. When the ratio of the harpagoside content (wt%) to the stachyose content (wt%) is within the above range, the devil's claw extract of the present invention is less likely to cause coloration or odor, has excellent stability, and is highly soluble, making it easy to incorporate into various products.
本発明のデビルズクロー抽出物は、液体でもよく、液体をスプレードライにより乾燥粉末としたものでもよい。本発明のデビルズクロー抽出物が液体である場合には、抽出溶媒が含まれていてもよい。上記抽出溶媒としては、水の他、メタノール、エタノール、プロパノール、イソプロパノール等の低級アルコール、1,3-ブチレングリコール、プロピレングリコール、ジプロピレングリコール、グリセリン等の多価アルコール、エチルエーテル、プロピルエーテル等のエーテル類、酢酸エチル、酢酸ブチル等のエステル類、アセトン、エチルメチルケトン等のケトン類等の極性有機溶媒を用いることができ、これらより1種又は2種以上を選択して用いてもよい。有機溶媒の中では、特に、化粧品、医薬品、食品製造等に安全に用いることができ、かつ水に溶けやすいエタノールが好ましく、又はこれらを組み合わせて用いてもよい。なお、本発明のデビルズクロー抽出物は、上記抽出液を濃縮、乾固したものを極性溶媒に再度溶解したり、スプレードライにより乾燥粉末としたものを再度溶解したものでもよい。The devil's claw extract of the present invention may be a liquid, or may be a liquid dried powder by spray drying. When the devil's claw extract of the present invention is a liquid, it may contain an extraction solvent. As the extraction solvent, in addition to water, lower alcohols such as methanol, ethanol, propanol, and isopropanol, polyhydric alcohols such as 1,3-butylene glycol, propylene glycol, dipropylene glycol, and glycerin, ethers such as ethyl ether and propyl ether, esters such as ethyl acetate and butyl acetate, ketones such as acetone and ethyl methyl ketone, and other polar organic solvents may be used, and one or more of these may be selected and used. Among the organic solvents, ethanol is particularly preferable because it can be safely used in cosmetics, pharmaceuticals, food production, and the like, and is easily soluble in water, or these may be used in combination. The devil's claw extract of the present invention may be obtained by concentrating and drying the above extract and dissolving it in a polar solvent again, or by dissolving it in a dried powder by spray drying again.
本発明のデビルズクロー抽出物が乾燥粉末である場合、乾燥粉末化する過程で添加されたデキストリン等の粉末化基材、カゼインソーダ、ホエー、ゼラチン、乳類、卵白等の蛋白質、庶糖、乳糖等の少糖類、アラビアガム、澱粉又はその分解物等が含まれていてもよい。When the devil's claw extract of the present invention is in the form of a dry powder, it may contain a powder base material such as dextrin, which is added during the drying and powdering process, protein such as casein sodium, whey, gelatin, milk, egg white, oligosaccharides such as sucrose and lactose, gum arabic, starch or hydrolyzates thereof, etc.
(特性)
本発明のデビルズクロー抽出物のpHは、通常2.0~10.0であり、3.0~9.0であることが好ましく、4.0~8.0であることがより好ましく、5.0~7.5であることがさらに好ましい。
(Characteristic)
The pH of the devil's claw extract of the present invention is usually 2.0 to 10.0, preferably 3.0 to 9.0, more preferably 4.0 to 8.0, and even more preferably 5.0 to 7.5.
本発明のデビルズクロー抽出物は、従来のデビルズクロー抽出物と比較して、着色が顕著に抑えられていることも特徴とひとつである。具体的には、本発明のデビルズクロー抽出物が乾燥粉末である場合、又はデビルズクロー抽出物が液体である場合にはそれを乾燥粉末とした場合、その0.5重量%濃度の水溶液の、可視光領域の波長における吸光度が0.1以下となる。上記可視光領域とは、400nm~500nmの波長をいう。上記吸光度は、0.08以下であることが好ましく、0.05以下であることがより好ましく、0.03以下であることがさらに好ましい。One of the features of the devil's claw extract of the present invention is that coloring is significantly suppressed compared to conventional devil's claw extracts. Specifically, when the devil's claw extract of the present invention is a dry powder, or when the devil's claw extract is a liquid and is made into a dry powder, the absorbance of a 0.5% by weight aqueous solution in the visible light region is 0.1 or less. The visible light region refers to wavelengths from 400 nm to 500 nm. The absorbance is preferably 0.08 or less, more preferably 0.05 or less, and even more preferably 0.03 or less.
さらに、本発明のデビルズクロー抽出物は、従来のデビルズクロー抽出物と比較して、長期保存後の着色変化が顕著に抑えられ、安定性にも優れる。そのため、本発明のデビルズクロー抽出物は原料として、又はそれを含む製品としての保管期間を長期とすることが可能である。 Furthermore, the devil's claw extract of the present invention is more stable and undergoes less color change after long-term storage than conventional devil's claw extracts. Therefore, the devil's claw extract of the present invention can be stored for a long period of time as a raw material or as a product containing the same.
本発明のデビルズクロー抽出物は、従来のデビルズクロー抽出物と比較して、ハルパゴシド特有の臭いが顕著に抑えられている。具体的には、精製水を陰性対照として官能試験を行うことで確認することができる。 Compared to conventional devil's claw extracts, the devil's claw extract of the present invention has a significantly reduced odor characteristic of harpagoside. Specifically, this can be confirmed by conducting a sensory test using purified water as a negative control.
本発明のデビルズクロー抽出物は、従来のデビルズクロー抽出物と比較して、水溶性溶媒に対する溶解度が高いので、透過度が精製水と同程度であり、透明性に優れる。そのため、化粧品、飲料等の様々な製品に使用することが可能となる。The devil's claw extract of the present invention has a higher solubility in water-soluble solvents than conventional devil's claw extracts, and therefore has a transmittance equivalent to that of purified water and excellent transparency. This makes it possible to use it in a variety of products such as cosmetics and beverages.
(作用効果及び用途)
本発明のデビルズクロー抽出物は、細胞内のメラニン合成酵素遺伝子の発現を抑制する作用を有する。上記メラニン合成酵素遺伝子としては、例えは、TYR(Tyrosinase,TYR)、TYRP1(Tyrosinase related protein 1)、DCT(Dopachrome tautomerase)等が挙げられる。本発明のデビルズクロー抽出物をメラノサイト等の細胞に作用させると、上記メラニン合成酵素遺伝子の発現を抑制することができる。したがって、本発明のデビルズクロー抽出物は、美白効果を有し、日焼けや、エイジングによるシミ・くすみを改善することができる。即ち、本発明のデビルズクロー抽出物はメラニン合成酵素遺伝子発現抑制用組成物、メラニン合成酵素遺伝子発現抑制剤、美白用組成物、美白剤として好適に使用することができる。
(Effects and uses)
The devil's claw extract of the present invention has an effect of suppressing the expression of melanin synthesis enzyme genes in cells. Examples of the melanin synthesis enzyme genes include TYR (Tyrosinase, TYR), TYRP1 (Tyrosinase related protein 1), and DCT (Dopachrome tautomerase). When the devil's claw extract of the present invention is applied to cells such as melanocytes, the expression of the melanin synthesis enzyme genes can be suppressed. Therefore, the devil's claw extract of the present invention has a whitening effect and can improve age spots and dullness caused by sunburn or aging. That is, the devil's claw extract of the present invention can be suitably used as a composition for suppressing the expression of melanin synthesis enzyme genes, a melanin synthesis enzyme gene expression inhibitor, a whitening composition, and a whitening agent.
本発明のデビルズクロー抽出物は、線維芽細胞等の各種細胞のコラーゲン産生能を向上させる作用、即ちコラーゲン産生促進作用を有する。このコラーゲン産生促進作用は、本発明のデビルズクロー抽出物が含有するスクロース、スタキオース、ラフィノース等の多糖類による効果が組み合わさって得られるものである可能性が考えられる。本発明のデビルズクロー抽出物は、細胞からのコラーゲン産生を促進させることで、シワ・たるみに対して優れた効果を示す抗シワ、アンチエイジング素材として、またコラーゲン産生促進用組成物、コラーゲン産生促進剤として、種々の製品において好適に使用することができる。The devil's claw extract of the present invention has the effect of improving the collagen production ability of various cells such as fibroblasts, i.e., collagen production promoting effect. It is considered possible that this collagen production promoting effect is obtained by combining the effects of polysaccharides such as sucrose, stachyose, and raffinose contained in the devil's claw extract of the present invention. The devil's claw extract of the present invention can be suitably used in various products as an anti-wrinkle and anti-aging material that is highly effective against wrinkles and sagging by promoting collagen production from cells, as a composition for promoting collagen production, and as a collagen production promoter.
本発明のデビルズクロー抽出物は、線維芽細胞等の各種細胞によるエラスチン線維形成促進作用を有する。本発明のデビルズクロー抽出物はシワ・たるみに効果を示す抗シワ、アンチエイジング素材として、またエラスチン線維形成促進用組成物、エラスチン線維形成促進剤として、種々の製品において好適に使用することができる。The devil's claw extract of the present invention has the effect of promoting elastin fiber formation by various cells such as fibroblasts. The devil's claw extract of the present invention can be suitably used in various products as an anti-wrinkle and anti-aging material that is effective against wrinkles and sagging, as a composition for promoting elastin fiber formation, and as an elastin fiber formation promoter.
本発明のデビルズクロー抽出物は、線維芽細胞、軟骨細胞等の各種細胞のヒアルロン酸産生能を向上させる作用、即ちヒアルロン酸産生促進作用を有する。本発明のデビルズクロー抽出物は、細胞からのヒアルロン酸産生を促進させることで、シワ・たるみに対して優れた効果を示す抗シワ、アンチエイジング素材として好適に使用することができる。また、加齢に伴う関節の痛みの原因の一つにヒアルロン酸など関節成分の減少が挙げられるが、本発明のデビルズクロー抽出物の摂取によって関節痛を弱める効果が期待される。本発明のデビルズクロー抽出物は、ヒアルロン酸産生促進用組成物、ヒアルロン酸産生促進剤として、種々の製品において好適に使用することができる。The devil's claw extract of the present invention has an effect of improving the hyaluronic acid production ability of various cells such as fibroblasts and chondrocytes, i.e., an effect of promoting hyaluronic acid production. The devil's claw extract of the present invention can be suitably used as an anti-wrinkle and anti-aging material that shows excellent effects against wrinkles and sagging by promoting the production of hyaluronic acid from cells. In addition, one of the causes of joint pain associated with aging is a decrease in joint components such as hyaluronic acid, and it is expected that the ingestion of the devil's claw extract of the present invention will have an effect of reducing joint pain. The devil's claw extract of the present invention can be suitably used in various products as a composition for promoting hyaluronic acid production and a hyaluronic acid production promoter.
本発明のデビルズクロー抽出物は、大気汚染物質により誘発される炎症性物質の産生抑制効果を有する。即ち、本発明のデビルズクロー抽出物は、Gobi Kosa Dust、PM2.5等の大気汚染物質により誘発される、(ヒト正常皮膚)表皮細胞、(ヒト)角膜上皮細胞等の各種細胞からの炎症性物質の産生を抑制する作用を有する。そのため、本発明のデビルズクロー抽出物は抗炎症用組成物、特に大気汚染物質により誘発される炎症用の抗炎症組成物、大気汚染物質により誘発される皮膚障害(バリア機能低下も含む)改善用組成物、皮膚のバリア機能亢進用組成物、アンチポリューション組成物として、種々の製品において好適に使用することができる。The devil's claw extract of the present invention has an effect of suppressing the production of inflammatory substances induced by air pollutants. That is, the devil's claw extract of the present invention has an effect of suppressing the production of inflammatory substances from various cells such as (human normal skin) epidermal cells and (human) corneal epithelial cells, which are induced by air pollutants such as Gobi Kosa Dust and PM2.5. Therefore, the devil's claw extract of the present invention can be suitably used in various products as an anti-inflammatory composition, particularly an anti-inflammatory composition for inflammation induced by air pollutants, a composition for improving skin disorders (including reduced barrier function) induced by air pollutants, a composition for enhancing the barrier function of the skin, and an anti-pollution composition.
[デビルズクロー抽出物の製造方法]
本発明のデビルズクロー抽出物の製造方法は、(A)デビルズクロー乾燥粉末の抽出液を得る工程、及び(B)上記抽出液を、疎水性成分を吸着させる樹脂で処理して精製抽出液を得る工程を含む。さらに、(C)粉末化工程、(D)粉末の再溶解工程を有していてもよい。各工程について、以下に詳細に説明する。
[Method of producing devil's claw extract]
The method for producing the Devil's Claw extract of the present invention includes (A) a step of obtaining an extract of the Devil's Claw dry powder, and (B) a step of treating the extract with a resin capable of adsorbing hydrophobic components to obtain a purified extract. The method may further include (C) a powdering step, and (D) a powder redissolving step. Each step will be described in detail below.
(A)デビルズクロー乾燥粉末の抽出液を得る工程
デビルズクローの塊茎部分の乾燥物を、必要によりミキサー等で裁断、粉砕する。これを抽出溶媒で抽出する。上記抽出溶媒としては、水の他、メタノール、エタノール、プロパノール、イソプロパノール等の低級アルコール、1,3-ブチレングリコール、プロピレングリコール、ジプロピレングリコール、グリセリン等の多価アルコール、エチルエーテル、プロピルエーテル等のエーテル類、酢酸エチル、酢酸ブチル等のエステル類、アセトン、エチルメチルケトン等のケトン類等の極性有機溶媒を用いることができ、これらより1種又は2種以上を選択して用いてもよい。有機溶媒の中では、特に、化粧品、医薬品、食品製造等に安全に用いることができ、かつ水に溶けやすいエタノールが好ましく、又はこれらを組み合わせて用いてもよく、例えば30%~70%(W/W)エタノール水溶液、50%(W/W)エタノール水溶液をより好ましく用いることができる。
(A) Step of Obtaining Extract of Devil's Claw Dry Powder Dried Devil's Claw tubers are cut and pulverized with a mixer or the like as necessary. This is extracted with an extraction solvent. As the extraction solvent, in addition to water, polar organic solvents such as lower alcohols such as methanol, ethanol, propanol, and isopropanol, polyhydric alcohols such as 1,3-butylene glycol, propylene glycol, dipropylene glycol, and glycerin, ethers such as ethyl ether and propyl ether, esters such as ethyl acetate and butyl acetate, and ketones such as acetone and ethyl methyl ketone can be used, and one or more of these may be selected and used. Among the organic solvents, ethanol is particularly preferable because it can be safely used in cosmetics, pharmaceuticals, food production, and the like and is easily soluble in water, or these may be used in combination, and for example, a 30% to 70% (W/W) ethanol aqueous solution or a 50% (W/W) ethanol aqueous solution can be more preferably used.
上記抽出の際の温度は特に限定されないが、抽出効率を向上させる観点から加熱抽出が好ましい。加熱温度としては、40℃~100℃が好ましく、50℃~90℃がより好ましい。抽出時間は、抽出時の温度により適宜変更できるが、加熱抽出の場合には通常0.5時間~48時間であり、1時間~15時間が好ましく、1.5時間~10時間がより好ましい。また、常温抽出の場合には、通常2日~20日であり、5日~15日が好ましく、8日~12日がより好ましい。抽出の間は、撹拌することで抽出の効率を向上させることができる。抽出後、活性炭等で処理を行ってもよい。その後、濾紙等で濾過して抽出液を得る。The temperature during the above extraction is not particularly limited, but from the viewpoint of improving the extraction efficiency, heated extraction is preferred. The heating temperature is preferably 40°C to 100°C, more preferably 50°C to 90°C. The extraction time can be changed appropriately depending on the temperature during extraction, but in the case of heated extraction, it is usually 0.5 hours to 48 hours, preferably 1 hour to 15 hours, and more preferably 1.5 hours to 10 hours. In addition, in the case of room temperature extraction, it is usually 2 days to 20 days, preferably 5 days to 15 days, and more preferably 8 days to 12 days. The efficiency of the extraction can be improved by stirring during the extraction. After extraction, treatment with activated carbon or the like may be performed. The extract is then obtained by filtration with filter paper or the like.
(B)上記抽出液を、疎水性成分を吸着させる樹脂で処理して精製抽出液を得る工程
本工程においては、上記抽出液をカラム精製して精製抽出液を取得する。上記カラムとしては、ハルパゴシド等の疎水性成分を吸着させることができる樹脂から構成されるカラムを用いることができる。そのような樹脂としては、疎水性成分を吸着させることができるものであれば特に限定されないが、例えばダイヤイオン(登録商標)HP20、HP21、HP20SS、;セパビーズ(登録商標)SP825L、SP850、SP700、SP70、SP207、SP207SS、SP20SS等の芳香族系合成吸着剤、ダイヤイオン(登録商標)HP2MGL、HP2MGS等のメタクリル系合成吸着剤(いずれも三菱ケミカル社製)等が挙げられる。なお、本工程における精製は、上記樹脂を用いたバッチ精製としてもよい。上記樹脂から構成されるカラムによる精製及びバッチ精製は、それぞれの樹脂に適した方法で、仕様書等に従い行うことができる。本工程により、(A)工程で得られた抽出液から疎水性成分の一部又は全部が除去された精製抽出液を得ることができる。
(B) A step of treating the extract with a resin that adsorbs hydrophobic components to obtain a purified extract In this step, the extract is purified through a column to obtain a purified extract. As the column, a column composed of a resin capable of adsorbing hydrophobic components such as harpagoside can be used. Such resins are not particularly limited as long as they can adsorb hydrophobic components, and examples thereof include aromatic synthetic adsorbents such as Diaion (registered trademark) HP20, HP21, and HP20SS; Sepabeads (registered trademark) SP825L, SP850, SP700, SP70, SP207, SP207SS, and SP20SS; and methacrylic synthetic adsorbents such as Diaion (registered trademark) HP2MGL and HP2MGS (all manufactured by Mitsubishi Chemical Corporation). The purification in this step may be batch purification using the resin. Purification using a column composed of the resin and batch purification can be performed according to the specifications and the like by a method suitable for each resin. This step makes it possible to obtain a purified extract from the extract obtained in step (A) in which a part or all of the hydrophobic components have been removed.
(C)粉末化工程
本工程においては、(B)工程で得られた精製抽出液を粉末とする。精製抽出液を粉末にする方法としては、例えば凍結乾燥法、スプレードライ法、濃縮・乾固による方法等が挙げられる。
(C) Powdering Step In this step, the purified extract obtained in step (B) is powdered. Examples of methods for powdering the purified extract include freeze-drying, spray-drying, and concentration/drying.
(D)粉末の再溶解工程
本工程においては、(C)工程で得られた粉末を溶媒に再度溶解する。上記溶媒としては、水の他、メタノール、エタノール、プロパノール、イソプロパノール等の低級アルコール、1,3-ブチレングリコール、プロピレングリコール、ジプロピレングリコール、グリセリン等の多価アルコール、エチルエーテル、プロピルエーテル等のエーテル類、酢酸エチル、酢酸ブチル等のエステル類、アセトン、エチルメチルケトン等のケトン類等の極性有機溶媒を用いることができ、これらより1種又は2種以上を選択して用いてもよい。これらのうち、1,3-ブチレングリコール、プロピレングリコール、ジプロピレングリコール等が好ましく、1,3-ブチレングリコールがより好ましい。
(D) Powder redissolving step In this step, the powder obtained in step (C) is redissolved in a solvent. As the solvent, in addition to water, polar organic solvents such as lower alcohols such as methanol, ethanol, propanol, and isopropanol, polyhydric alcohols such as 1,3-butylene glycol, propylene glycol, dipropylene glycol, and glycerin, ethers such as ethyl ether and propyl ether, esters such as ethyl acetate and butyl acetate, and ketones such as acetone and ethyl methyl ketone can be used, and one or more of these may be selected and used. Among these, 1,3-butylene glycol, propylene glycol, dipropylene glycol, and the like are preferred, and 1,3-butylene glycol is more preferred.
本発明の製造方法により得られた本発明のデビルズクロー抽出物は、上記工程を経ることで、従来のデビルズクロー抽出物から、有効成分として知られていたハルパゴシド等の疎水性の物質が除去され、各成分の効果が適度に組み合わされることで、上述した様々な効果を奏することができる。The devil's claw extract of the present invention obtained by the manufacturing method of the present invention undergoes the above-mentioned steps to remove hydrophobic substances such as harpagoside, which were known to be active ingredients in conventional devil's claw extracts, and the effects of each component are appropriately combined to provide the various effects described above.
なお、上記(A)工程によって得られるデビルズクロー抽出液は、消炎鎮痛効果以外に、皮膚におけるメラニン合成酵素遺伝子発現抑制作用、コラーゲン産生促進作用、エラスチン線維形成促進作用、ヒアルロン酸産生促進作用、大気汚染物質により誘発される炎症性物質(IL-6、IL-8等)の産生抑制効果、大気汚染物質により誘発される皮膚障害(バリア機能低下も含む)改善効果等を有し、美白、抗シワ、アンチエイジング、関節症への効果、抗炎症効果(アンチポリューション)も期待できる。工程(A)によって得られるデビルズクロー抽出物も、着色等の問題はあるものの、化粧品、医薬品、医薬部外品食品(機能性食品、サプリメント、ドリンク剤等)等として、またその形態としては外用組成物、経口用組成物(食品組成物を含む)、眼科用組成物等として使用することができる。なお、上記(A)工程によって得られるデビルズクロー抽出液は、苦味を有しかつ様々な薬理効果を有することが知られているハルパゴシド等のイリドイド類が含まれているため、投与経路、適用部位、または適用対象によっては、不都合が生じることがある。In addition to the anti-inflammatory and analgesic effects, the devil's claw extract obtained by the above step (A) has the effect of suppressing the expression of melanin synthesis enzyme genes in the skin, promoting collagen production, promoting the formation of elastin fibers, promoting the production of hyaluronic acid, suppressing the production of inflammatory substances (IL-6, IL-8, etc.) induced by air pollutants, improving skin disorders (including impaired barrier function) induced by air pollutants, and is expected to have whitening, anti-wrinkle, anti-aging, arthropathy, and anti-inflammatory effects (anti-pollution). Although the devil's claw extract obtained by step (A) has problems such as coloring, it can be used as cosmetics, medicines, quasi-drug foods (functional foods, supplements, drinks, etc.), and in the form of external compositions, oral compositions (including food compositions), ophthalmic compositions, etc. In addition, since the devil's claw extract obtained by the above step (A) contains iridoids such as harpagoside, which are known to have a bitter taste and various pharmacological effects, inconveniences may occur depending on the administration route, application site, or application subject.
[デビルズクロー抽出物を含有する各種組成物、各種剤]
上述のとおり、本発明のデビルズクロー抽出物はメラニン合成酵素遺伝子発現抑制作用を有することから、本発明のデビルズクロー抽出物を含有する組成物は、メラニン合成酵素遺伝子発現抑制用組成物、メラニン合成酵素遺伝子発現抑制剤、美白用組成物、美白剤として使用できる。本発明は、本発明のデビルズクロー抽出物を含有する、メラニン合成酵素遺伝子発現抑制用組成物、メラニン合成酵素遺伝子発現抑制剤、美白用組成物、美白剤も含む。
[Various compositions and agents containing Devil's Claw extract]
As described above, the devil's claw extract of the present invention has an inhibitory effect on the expression of melanin synthesis enzyme genes, and therefore a composition containing the devil's claw extract of the present invention can be used as a composition for inhibiting the expression of melanin synthesis enzyme genes, an inhibitor of melanin synthesis enzyme gene expression, a composition for whitening, or a whitening agent. The present invention also includes a composition for inhibiting the expression of melanin synthesis enzyme genes, an inhibitor of melanin synthesis enzyme gene expression, a composition for whitening, or a whitening agent, each of which contains the devil's claw extract of the present invention.
上述のとおり、本発明のデビルズクロー抽出物は、各種細胞に対してコラーゲン産生促進作用を示すことから、本発明のデビルズクロー抽出物を含有する組成物は、コラーゲン産生促進用組成物、コラーゲン産生促進剤として使用できる。本発明は、本発明のデビルズクロー抽出物を含有するコラーゲン産生促進用組成物、コラーゲン産生促進剤も含む。As described above, the devil's claw extract of the present invention exhibits a collagen production promoting effect on various cells, and therefore a composition containing the devil's claw extract of the present invention can be used as a collagen production promoting composition or collagen production promoter. The present invention also includes a collagen production promoting composition or collagen production promoter containing the devil's claw extract of the present invention.
上述のとおり、本発明のデビルズクロー抽出物は、線維芽細胞等に対してエラスチン線維形成促進作用を有することから、本発明のデビルズクロー抽出物を含有する組成物は、エラスチン線維形成促進用組成物、エラスチン線維形成促進剤として使用できる。本発明は、本発明のデビルズクロー抽出物を含有するエラスチン線維形成促進用組成物、エラスチン線維形成促進剤も含む。As described above, the devil's claw extract of the present invention has an elastin fiber formation promoting effect on fibroblasts and the like, and therefore a composition containing the devil's claw extract of the present invention can be used as a composition for promoting elastin fiber formation and an elastin fiber formation promoter. The present invention also includes a composition for promoting elastin fiber formation and an elastin fiber formation promoter that contain the devil's claw extract of the present invention.
上述のとおり、本発明のデビルズクロー抽出物は各種細胞のヒアルロン酸産生促進作用を有することから、本発明のデビルズクロー抽出物を含有する組成物は、ヒアルロン酸産生促進用組成物、ヒアルロン酸産生促進剤として使用できる。また、関節症の緩和・改善用組成物としても使用できる。本発明は、本発明のデビルズクロー抽出物を含有するヒアルロン酸産生促進用組成物、ヒアルロン酸産生促進剤、関節症の緩和・改善用組成物も含む。As described above, the devil's claw extract of the present invention has the effect of promoting hyaluronic acid production in various cells, and therefore a composition containing the devil's claw extract of the present invention can be used as a composition for promoting hyaluronic acid production or as a hyaluronic acid production promoter. It can also be used as a composition for alleviating or improving arthropathy. The present invention also includes a composition for promoting hyaluronic acid production, a hyaluronic acid production promoter, and a composition for alleviating or improving arthropathy, each of which contains the devil's claw extract of the present invention.
上述のとおり、本発明のデビルズクロー抽出物は大気汚染物質により誘発される炎症性物質の産生抑制効果を有する。即ち、本発明のデビルズクロー抽出物は、Gobi Kosa Dust、PM2.5等の大気汚染物質により誘発される、(ヒト正常皮膚)表皮細胞、(ヒト)角膜上皮細胞等の各種細胞からの炎症性物質(IL-1β、IL-6、IL-8等)の産生を抑制する作用を有することから、本発明は、本発明のデビルズクロー抽出物を含有する抗炎症用組成物、特に大気汚染物質により誘発される炎症用の抗炎症組成物、大気汚染物質による皮膚障害(バリア機能低下も含む)改善用組成物、皮膚のバリア機能亢進用組成物、アンチポリューション組成物を含む。As described above, the devil's claw extract of the present invention has an effect of suppressing the production of inflammatory substances induced by air pollutants. That is, the devil's claw extract of the present invention has an effect of suppressing the production of inflammatory substances (IL-1β, IL-6, IL-8, etc.) from various cells such as (human normal skin) epidermal cells and (human) corneal epithelial cells, which are induced by air pollutants such as Gobi Kosa Dust and PM2.5. Therefore, the present invention includes an anti-inflammatory composition containing the devil's claw extract of the present invention, in particular an anti-inflammatory composition for inflammation induced by air pollutants, a composition for improving skin disorders (including impaired barrier function) caused by air pollutants, a composition for enhancing the barrier function of the skin, and an anti-pollution composition.
本発明のデビルズクロー抽出物を含有するメラニン合成酵素遺伝子発現抑制用組成物、メラニン合成酵素遺伝子発現抑制剤、美白用組成物、美白剤、コラーゲン産生促進用組成物、コラーゲン産生促進剤、エラスチン線維形成促進用組成物、エラスチン線維形成促進剤、ヒアルロン酸産生促進用組成物、ヒアルロン酸産生促進剤、抗炎症組成物、抗炎症剤、皮膚のバリア機能亢進用組成物、皮膚のバリア機能亢進剤、アンチポリューション組成物、アンチポリューション剤、大気汚染物質誘発炎症用の抗炎症組成物、大気汚染物質誘発炎症用の抗炎症剤、大気汚染物質による皮膚障害改善用組成物、大気汚染物質による皮膚障害改善剤、Gobi Kosa Dust誘発炎症用の抗炎症組成物、Gobi Kosa Dust誘発炎症用の抗炎症剤、関節症の緩和・改善用組成物、関節症の緩和・改善剤、炎症性物質発現抑制用組成物、炎症性物質発現抑制剤、IL-1β、IL-6又はIL-8発現抑制用組成物、IL-1β、IL-6又はIL-8発現抑制剤等の組成物は、外用又は内服など様々な形態に適用できる。即ち、上述の各種組成物及び各種剤は、外用組成物であってもよいし、内服用組成物、食品組成物等の経口用組成物(アイケアサプリ等も含む)、点眼剤や眼洗浄剤、眼軟膏等の眼科用組成物であってもよい。具体的には、医薬品、医薬部外品、局所(手、足、膝、ひじ、かかと、顔、目周り等)又は全身用の皮膚化粧料や皮膚洗浄剤、頭皮・頭髪に適用する薬用又は化粧用の製剤類をはじめとする各種の皮膚外用剤、浴用剤、経口摂取する医薬品・医薬部外品の内服用組成物、点眼等による医薬品・医薬部外品(洗眼剤、眼軟膏を含む)、一般的な飲食品、サプリメントやドリンク剤、機能性食品として使用することができる。 A composition for suppressing melanin synthesis enzyme gene expression, melanin synthesis enzyme gene expression inhibitor, skin whitening composition, skin whitening agent, composition for promoting collagen production, collagen production promoter, composition for promoting elastin fiber formation, elastin fiber formation promoter, composition for promoting hyaluronic acid production, hyaluronic acid production promoter, anti-inflammatory composition, anti-inflammatory agent, composition for enhancing skin barrier function, skin barrier function enhancer, anti-pollution composition, anti-pollution agent, anti-inflammatory composition for inflammation induced by air pollutants, anti-inflammatory agent for inflammation induced by air pollutants, composition for improving skin disorders caused by air pollutants, agent for improving skin disorders caused by air pollutants, anti-inflammatory composition for inflammation induced by Gobi Kosa Dust, Gobi Kosa Compositions such as an anti-inflammatory agent for Dust-induced inflammation, a composition for alleviating/improving arthropathy, an agent for alleviating/improving arthropathy, a composition for suppressing the expression of an inflammatory substance, an inhibitor of the expression of an inflammatory substance, a composition for suppressing the expression of IL-1β, IL-6 or IL-8, an inhibitor of the expression of IL-1β, IL-6 or IL-8, etc., can be applied in various forms such as external application or internal administration. That is, the above-mentioned various compositions and agents may be external compositions, internal compositions, oral compositions such as food compositions (including eye care supplements, etc.), and ophthalmic compositions such as eye drops, eye cleansers, and eye ointments. Specifically, they can be used as medicines, quasi-drugs, skin cosmetics and skin cleansers for local (hands, feet, knees, elbows, heels, face, around the eyes, etc.) or whole body use, various external skin preparations including medicinal or cosmetic preparations for application to the scalp and hair, bath additives, oral compositions for taking medicines and quasi-drugs, medicines and quasi-drugs (including eye washes and eye ointments) for eye drops, general foods and beverages, supplements and drinks, and functional foods.
本発明のデビルズクロー抽出物を含有する各種組成物及び各種剤におけるデビルズクロー抽出物の含有量は、その剤型、用途によって適宜調整すればよく、特に制限はないが、一般的には、デビルズクロー抽出物に含有されるスタキオースの量に換算して、0.00001重量%~10重量%であり、0.00005重量%~5重量%であることが好ましく、0.0001~2重量%であることがより好ましく、0.0005~2重量%であることがさらにより好ましい。The content of devil's claw extract in various compositions and agents containing the devil's claw extract of the present invention may be adjusted appropriately depending on the dosage form and purpose, and is not particularly limited; however, generally, in terms of the amount of stachyose contained in the devil's claw extract, it is 0.00001% to 10% by weight, preferably 0.00005% to 5% by weight, more preferably 0.0001 to 2% by weight, and even more preferably 0.0005 to 2% by weight.
本発明のデビルズクロー抽出物を含有する上記の各種組成物、各種剤は、必須成分であるデビルズクロー抽出物以外に、本発明の効果を損なわない範囲でその他の成分を含んでもよい。例えば、通常の外用又は内用素材への処理等で使用されている薬剤等と組み合わせて使用することができ、併用薬剤により本発明の効果がより発現しやすくなる組合わせは好ましい。The above-mentioned various compositions and agents containing the devil's claw extract of the present invention may contain other ingredients in addition to the essential ingredient devil's claw extract, as long as the ingredients do not impair the effects of the present invention. For example, they can be used in combination with drugs and the like that are normally used in treating materials for external or internal use, and combinations in which the effects of the present invention are more easily achieved by using the combined drugs are preferred.
これらの他の成分としては、例えば、抗炎症剤(本発明のデビルズクロー抽出物を除く)、清涼化剤、抗菌・殺菌剤、ビタミン類、有機酸、糖類、保湿成分、多価アルコール、スクラブ剤、紫外線吸収成分、紫外線散乱成分、収斂成分、ペプチド又はその誘導体、アミノ酸又はその誘導体、洗浄成分、角質柔軟成分、細胞賦活化成分、老化防止成分、抗糖化成分、血行促進作用成分、美白成分、充血除去成分、眼筋調節薬成分、抗ヒスタミン薬成分又は抗アレルギー薬成分、ポリフェノール類等が挙げられる。なお、本発明の上記各種組成物、各種剤において、これらの成分はそれぞれ1種単独で用いてもよいし、2種以上を併用してもよい。 Examples of these other ingredients include anti-inflammatory agents (excluding the devil's claw extract of the present invention), cooling agents, antibacterial and disinfectant agents, vitamins, organic acids, sugars, moisturizing ingredients, polyhydric alcohols, scrubbing agents, UV absorbing ingredients, UV scattering ingredients, astringent ingredients, peptides or derivatives thereof, amino acids or derivatives thereof, cleansing ingredients, keratin softening ingredients, cell activating ingredients, anti-aging ingredients, anti-glycation ingredients, blood circulation promoting ingredients, whitening ingredients, congestion relief ingredients, ocular muscle regulating ingredients, antihistamine ingredients or antiallergic ingredients, polyphenols, etc. In the above-mentioned various compositions and agents of the present invention, each of these ingredients may be used alone or in combination of two or more kinds.
上記抗炎症剤としては、例えば、植物(例えば、コンフリー、オウレン、ドクダミ、カミツレ、ビルベリー、イザヨイバラ、エンメイソウ、ビワ、ニガハッカ、グリセリルグルコシド、ローヤルゼリー、メリアアザジラクタ、ゼニアオイ、オウゴン、シャクヤク、チンピ)に由来する成分、アラントイン及びその誘導体、グリチルレチン酸及びその誘導体、グリチルリチン酸及びその誘導体、サリチル酸誘導体、アミノカプロン酸、アズレン及びその誘導体、酸化亜鉛、カラミン、トラネキサム酸、ウフェナマート、ブフェキサマク、イブプロフェンピコノール、塩酸ピリドキシン、メントール、カンフル、テレピン油、インドメタシン、アゼライン酸、酢酸トコフェロール、ヒドロコルチゾン、プレドニゾロン並びにこれらの塩等が挙げられる。中でもアラントイン、グリチルレチン酸、グリチルリチン酸ジカリウム、アミノカプロン酸、アズレン及びその誘導体、酢酸トコフェロール、トラネキサム酸、ビルベリー葉エキス、チンピエキス、イザヨイバラエキス、ゼニアオイ花エキス、ドクダミエキスとの組み合わせが好ましい。Examples of the anti-inflammatory agents include components derived from plants (e.g., comfrey, coptis japonica, houttuynia cordata, chamomile, bilberry, rose rosa, emmeisou, loquat, horehound, glyceryl glucoside, royal jelly, melia azadirachta, mallow, scutellaria, peony, and tangerine), allantoin and its derivatives, glycyrrhetinic acid and its derivatives, glycyrrhizic acid and its derivatives, salicylic acid derivatives, aminocaproic acid, azulene and its derivatives, zinc oxide, calamine, tranexamic acid, ufenamate, bufexamac, ibuprofen piconol, pyridoxine hydrochloride, menthol, camphor, turpentine oil, indomethacin, azelaic acid, tocopherol acetate, hydrocortisone, prednisolone, and salts thereof. Among these, combinations with allantoin, glycyrrhetinic acid, dipotassium glycyrrhizinate, aminocaproic acid, azulene and its derivatives, tocopherol acetate, tranexamic acid, bilberry leaf extract, tangerine peel extract, Rosa rosa extract, mallow flower extract, and Houttuynia cordata extract are preferred.
上記清涼化剤としては、例えば、メントール及びその誘導体、カンフル、ボルネオール、ゲラニオール、シネオール、アネトール、リモネン、オイゲノール等のテルペン類(これらはd体、l体又はdl体のいずれでもよい。);ユーカリ油、ベルガモット油、ペパーミント油、クールミント油、スペアミント油、ウイキョウ油、ハッカ油、ケイヒ油、ローズ油、テレビン油等の精油等が挙げられる。中でも特にメントール及びその誘導体、カンフル、ユーカリ油、ペパーミント油、ハッカ油との組み合わせが好ましい。Examples of the cooling agents include menthol and its derivatives, camphor, borneol, geraniol, cineole, anethole, limonene, eugenol, and other terpenes (which may be in the d-, l-, or dl-form); and essential oils such as eucalyptus oil, bergamot oil, peppermint oil, cool mint oil, spearmint oil, fennel oil, peppermint oil, cinnamon oil, rose oil, and turpentine. Among these, combinations with menthol and its derivatives, camphor, eucalyptus oil, peppermint oil, and peppermint oil are particularly preferred.
上記抗菌・殺菌剤としては、例えば、イソプロピルメチルフェノール、クロルヘキシジン、サリチル酸、塩化ベンザルコニウム、アクリノール、エタノール、塩化ベンゼトニウム、クレゾール、グルコン酸及びその誘導体、ポピドンヨード、ヨウ化カリウム、ヨウ素、トリクロカルバン、トリクロサン、感光素101号、感光素201号、パラベン、フェノキシエタノール、炭素数5~10のアルカンジオール(例えば、1,2-ペンタンジオール、1,2-ヘキサンジオール、1,2-オクタンジオールなど)、塩酸アルキルジアミノグリシン、ピロクトオラミン、ミコナゾール若しくはその塩、塩化セチルトリメチルアンモニウム、ジンクピリチオン、塩化セチルピリジニウム、ミコナゾール、クロロブタノール、エチルヘキシルグリセリン、ブチルカルバミン酸ヨウ化プロピニル、カプリルヒドロキサム酸、フェネチルアルコール、ベンジルアルコール、メチルイソチアゾリノン、ソルビン酸、ソルビン酸カリウム、β-グリチルレチン酸、アゼライン酸、塩化ポリドロニウム、安息香酸ナトリウム、グルコン酸クロルヘキシジン、デヒドロ酢酸ナトリウム、パラオキシ安息香酸アルキル、硫酸オキシキノリン、ビグアニド化合物、植物(例えば、アロエ、クララ、ローズマリー、クワ、ユーカリ、キナ、チョウジなど)に由来する成分等が挙げられる。中でも特にイソプロピルメチルフェノール、サリチル酸、塩化ベンザルコニウム、エタノール、グルコン酸、パラベン、フェノキシエタノール、1,2-ペンタンジオール、1,2-ヘキサンジオール、アゼライン酸、エチルヘキシルグリセリン、ブチルカルバミン酸ヨウ化プロピニル、カプリルヒドロキサム酸、ローズマリーエキス、ユーカリエキス、アロエエキス、キナエキスとの組み合わせが好ましい。Examples of the antibacterial and disinfectant agents include isopropylmethylphenol, chlorhexidine, salicylic acid, benzalkonium chloride, acrinol, ethanol, benzethonium chloride, cresol, gluconic acid and its derivatives, povidone-iodine, potassium iodide, iodine, triclocarban, triclosan, photosensitizer No. 101, photosensitizer No. 201, paraben, phenoxyethanol, alkanediols having 5 to 10 carbon atoms (e.g., 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, etc.), alkyldiaminoglycine hydrochloride, piroctoolamine, miconazole or a salt thereof, cetyltrimethylammonium chloride, Examples of the active ingredient include sorbitol, zinc pyrithione, cetylpyridinium chloride, miconazole, chlorobutanol, ethylhexylglycerin, iodopropynyl butylcarbamate, caprylhydroxamic acid, phenethyl alcohol, benzyl alcohol, methylisothiazolinone, sorbic acid, potassium sorbate, β-glycyrrhetinic acid, azelaic acid, polydonium chloride, sodium benzoate, chlorhexidine gluconate, sodium dehydroacetate, alkyl paraoxybenzoate, oxyquinoline sulfate, biguanide compounds, and ingredients derived from plants (e.g., aloe, sophora flavescens, rosemary, mulberry, eucalyptus, cinchona, clove, etc.). Among these, combinations with isopropylmethylphenol, salicylic acid, benzalkonium chloride, ethanol, gluconic acid, paraben, phenoxyethanol, 1,2-pentanediol, 1,2-hexanediol, azelaic acid, ethylhexylglycerin, iodopropynyl butylcarbamate, caprylhydroxamic acid, rosemary extract, eucalyptus extract, aloe extract, and cinchona extract are particularly preferred.
上記ビタミン類としては、水溶性ビタミン及び油溶性ビタミンのいずれであってもよく、例えば、ピリドキシン、ピリドキサール、ピリドキサミン、5’-リン酸ピリドキサール、及びそれらの塩(例えば、塩酸ピリドキシン、酢酸ピリドキシン、塩酸ピリドキサール、塩酸ピリドキサミン)等のビタミンB6類;パントテン酸、パントテン酸カルシウム、パントテニルアルコール(パンテノール)、D-パンテサイン、D-パンテチン、補酵素A、パントテニルエチルエーテル、及びそれらの塩等のパントテン酸類;ニコチン酸、ニコチン酸dl-α-トコフェロール、ニコチン酸ベンジル、ニコチン酸メチル、ニコチン酸β-ブトキシエチル、ニコチン酸1-(4-メチルフェニル)エチル、ニコチン酸アミド、及びそれらの塩等のニコチン酸類;γ-オリザノール、チアミン、ジベンゾイルチアミン、チアミンセチル、チアミンモノリン酸エステル、チアミンジリン酸エステル、チアミントリリン酸エステル、及びそれらの塩(例えば、ジベンゾイルチアミン塩酸塩、チアミン塩酸塩、チアミンセチル塩酸塩、チアミンチオシアン酸塩、チアミンラウリル塩酸塩、チアミン硝酸塩、チアミンモノリン酸塩、チアミンリジン塩、チアミントリリン酸塩、チアミンモノリン酸エステルリン酸塩、チアミンジリン酸エステル塩酸塩、チアミントリリン酸エステルモノリン酸塩)等のビタミンB1類;リボフラビン、フラビンモノヌクレオチド、フラビンアデニンジヌクレオチド、リボフラビン酪酸エステル、リボフラビンテトラ酪酸エステル、リボフラビン5’-リン酸エステルナトリウム、リボフラビンテトラニコチン酸エステル、及びそれらの塩等のビタミンB2類;ビオチン、ビオシチン、及びそれらの塩等のビオチン類;葉酸、プテロイルグルタミン酸、及びそれらの塩等の葉酸類;シアノコバラミン、ヒドロキソコバラミン、デオキシアデノシルコバラミン、及びそれらの塩等のビタミンB12類;アスコルビン酸、アスコルビン酸ナトリウム、デヒドロアスコルビン酸、アスコルビン酸リン酸エステル、アスコルビン酸硫酸エステル、アスコルビン酸-2-グルコシド、2-O-エチルアスコルビン酸、3-O-エチルアスコルビン酸、グリセリルアスコルビン酸、ビスグリセリルアスコルビン酸、アルキルグリセリルアスコルビン酸等のアスコルビン酸誘導体、及びそれらの塩(例えば、アスコルビン酸ナトリウム、アスコルビン酸リン酸エステルナトリウム、アスコルビン酸リン酸エステルマグネシウム)等の水溶性のビタミンC類、ステアリン酸アスコルビル、イソステアリルアスコルビルリン酸2ナトリウム、ジパルミチン酸L-アスコルビル、テトライソパルミチン酸アスコルビル(テトラ2-ヘキシルデカン酸アスコルビル)、パルミチン酸アスコルビルリン酸3ナトリウム等の油溶性または両親媒性のビタミンC類;δ-トコフェロール、dl-α-トコフェロール、酢酸dl-α-トコフェロール、コハク酸dl-α-トコフェロール、コハク酸dl-α-トコフェロールカルシウム、リノール酸トコフェロール、(リノール酸/オレイン酸)トコフェロール、トコフェロール、(アスコルビル/トコフェリル)リン酸カリウム、マレイン酸アスコルビルトコフェリル等のビタミンE類;アスコルビゲン-A、アスコルビン酸ステアリン酸エステル、アスコルビン酸パルミチン酸エステル、ジパルミチン酸L-アスコルビル、テトラ2-ヘキシルデカン酸アスコルビル等の油溶性のビタミンC及びその塩類;エルゴカルシフェロール、コレカルシフェロール等のビタミンD類;フィロキノン、ファルノキノン等のビタミンK類;レチノール、レチナール、レチノイン酸、3-デヒドロレチノール、3-デヒドロレチナール、3-デヒドロレチノイン酸、水添レチノールなどのビタミンA類及びその誘導体であるパルミチン酸レチノール、プロピオン酸レチノール、リノール酸レチノール、酢酸レチノール、レチノイン酸レチノール、d-δ-トコフェリルレチノエート、α-トコフェリルレチノエート、β-トコフェリルレチノエートなどのビタミンA誘導体類、α-カロテン、β-カロテン、γ-カロテン、クリプトキサンチン、リコピン、ゼアキサンチン、エキネノンなどのプロビタミンA類;フェルラ酸、ピロロキノリンキノン又はその塩、ヘスペリジン及びグルコシルヘルペリジン等のヘスペリジン誘導体、ユビキノン、グルクロラクトン、グルクロン酸アミド、オロチン酸、L-カルニチン、α-リポ酸、オロット酸等のビタミン様作用因子等が挙げられる。中でもビタミンB類、ビタミンC類、ビタミンE類、ビタミンA類、ビタミン様作用因子との組み合わせが好ましく、特に塩酸ピリドキシン、パントテニルアルコール(パンテノール)、ニコチン酸アミド、リボフラビン、シアノコバラミン、アスコルビン酸、アスコルビン酸リン酸エステル、アスコルビン酸-2-グルコシド、3-O-エチルアスコルビン、アスコルビン酸ナトリウム、アスコルビン酸リン酸エステルナトリウム、アスコルビン酸リン酸エステルマグネシウム、酢酸dl-α-トコフェロール、アスコルビン酸パルミチン酸エステル、テトラ2-ヘキシルデカン酸アスコルビル、レチノール、パルミチン酸レチノール、プロピオン酸レチノール、酢酸レチノール、ピロロキノリンキノン又はその塩、ユビキノン、γ-オリザノールから選ばれる1種又は2種以上との組み合わせがより好ましい。The vitamins may be either water-soluble or oil-soluble, for example, vitamin B6 such as pyridoxine, pyridoxal, pyridoxamine, 5'-pyridoxal phosphate, and salts thereof (e.g., pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, pyridoxamine hydrochloride); pantothenic acids such as pantothenic acid, calcium pantothenate, pantothenyl alcohol (panthenol), D-panthesine, D-pantethine, coenzyme A, pantothenyl ethyl ether, and salts thereof; nicotine nicotinic acids such as nicotinic acid, dl-α-tocopherol nicotinate, benzyl nicotinate, methyl nicotinate, β-butoxyethyl nicotinate, 1-(4-methylphenyl)ethyl nicotinate, nicotinamide, and salts thereof; γ-oryzanol, thiamine, dibenzoylthiamine, thiamine cetyl, thiamine monophosphate, thiamine diphosphate, thiamine triphosphate, and salts thereof (e.g., dibenzoylthiamine hydrochloride, thiamine hydrochloride, thiamine cetyl hydrochloride, thiamine thiocyanate, thiamine vitamin B1 such as thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine triphosphate, thiamine monophosphate phosphate, thiamine diphosphate hydrochloride, and thiamine triphosphate monophosphate; vitamin B2 such as riboflavin, flavin mononucleotide, flavin adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, riboflavin 5'-phosphate sodium, riboflavin tetranicotinate, and salts thereof; Biotins such as folic acid, pteroylglutamic acid, and salts thereof; folates such as folic acid, pteroylglutamic acid, and salts thereof; vitamin B12s such as cyanocobalamin, hydroxocobalamin, deoxyadenosylcobalamin, and salts thereof; ascorbic acid, sodium ascorbate, dehydroascorbic acid, ascorbic acid phosphate, ascorbic acid sulfate, ascorbic acid-2-glucoside, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, glyceryl ascorbic acid, bisglyceryl ascorbate, water-soluble vitamin C such as ascorbic acid, ascorbic acid derivatives such as alkyl glyceryl ascorbic acid, and salts thereof (e.g., sodium ascorbate, sodium ascorbyl phosphate, magnesium ascorbyl phosphate); oil-soluble or amphiphilic ascorbyl stearate, disodium isostearyl ascorbyl phosphate, L-ascorbyl dipalmitate, ascorbyl tetraisopalmitate (ascorbyl tetra 2-hexyldecanoate), trisodium ascorbyl palmitate phosphate, etc. Vitamin C such as δ-tocopherol, dl-α-tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol succinate, dl-α-tocopherol calcium succinate, tocopherol linoleate, tocopherol (linoleic acid/oleic acid), tocopherol, potassium (ascorbyl/tocopheryl) phosphate, and ascorbyl tocopheryl maleate; ascorbigen-A, ascorbyl stearate, ascorbyl palmitate, and L-ascorbyl dipalmitate. oil-soluble vitamin C and its salts, such as ascorbyl, tetra-2-hexyldecanoate, etc.; vitamin D, such as ergocalciferol, cholecalciferol, etc.; vitamin K, such as phylloquinone, falnoquinone, etc.; vitamin A, such as retinol, retinal, retinoic acid, 3-dehydroretinol, 3-dehydroretinal, 3-dehydroretinoic acid, hydrogenated retinol, etc., and their derivatives, such as retinol palmitate, retinol propionate, retinol linoleate, retinol acetate, retinol retinoic acid, d-δ-thiamine, etc. vitamin A derivatives such as tocopheryl retinoate, α-tocopheryl retinoate, β-tocopheryl retinoate, etc.; provitamin A such as α-carotene, β-carotene, γ-carotene, cryptoxanthin, lycopene, zeaxanthin, echinenone, etc.; hesperidin derivatives such as ferulic acid, pyrroloquinoline quinone or a salt thereof, hesperidin and glucosyl herperidin, etc.; vitamin-like action factors such as ubiquinone, glucurolactone, glucuronic acid amide, orotic acid, L-carnitine, α-lipoic acid, orotic acid, etc. Among these, combinations with B vitamins, C vitamins, E vitamins, A vitamins, and vitamin-like action factors are preferred, and combinations with one or more selected from pyridoxine hydrochloride, pantothenyl alcohol (panthenol), nicotinamide, riboflavin, cyanocobalamin, ascorbic acid, ascorbic acid phosphate, ascorbic acid-2-glucoside, 3-O-ethyl ascorbyl, sodium ascorbate, sodium ascorbyl phosphate, magnesium ascorbyl phosphate, dl-α-tocopherol acetate, ascorbyl palmitate, ascorbyl tetra-2-hexyldecanoate, retinol, retinol palmitate, retinol propionate, retinol acetate, pyrroloquinoline quinone or a salt thereof, ubiquinone, and γ-oryzanol are more preferred.
上記有機酸としては、例えば、グルコン酸、アスパラギン酸、アミノエチルスルホン酸、クエン酸、グルタミン酸、コハク酸、シュウ酸、フマル酸、マロン酸、マレイン酸、プロピオン酸、リンゴ酸、サリチル酸、グリコール酸、フィチン酸、酒石酸、酢酸、乳酸、パントテン酸、グリチルレチン酸、アルギン酸、アスコルビン酸、安息香酸、アジピン酸、グルタミン酸、アゼライン酸及びこれらの塩が挙げられる。塩としては、例えば、硫酸、塩酸又はリン酸等の鉱酸の塩、マレイン酸又はメタンスルホン酸等の有機酸の塩、ナトリウム又はカリウム等のアルカリ金属塩、アルカリ土類金属塩、亜鉛、銅、アンモニウム塩、塩基性アミノ酸塩、トリエタノールアミンのようなアミン塩等が挙げられる。好ましくは、アルカリ金属塩、アルカリ土類金属塩、アミン塩、亜鉛、銅から選ばれることが好ましく、ナトリウム、カリウム、トリエタノールアミン塩、亜鉛、銅がより好ましい。中でもグルコン酸、クエン酸、グルタミン酸、コハク酸、リンゴ酸、サリチル酸、グリコール酸、フィチン酸、酒石酸、乳酸、グリチルレチン酸から選ばれる1種又は2種以上との組み合わせがより好ましい。Examples of the organic acids include gluconic acid, aspartic acid, aminoethylsulfonic acid, citric acid, glutamic acid, succinic acid, oxalic acid, fumaric acid, malonic acid, maleic acid, propionic acid, malic acid, salicylic acid, glycolic acid, phytic acid, tartaric acid, acetic acid, lactic acid, pantothenic acid, glycyrrhetinic acid, alginic acid, ascorbic acid, benzoic acid, adipic acid, glutamic acid, azelaic acid, and salts thereof. Examples of the salts include salts of mineral acids such as sulfuric acid, hydrochloric acid, and phosphoric acid, salts of organic acids such as maleic acid and methanesulfonic acid, salts of alkali metals such as sodium and potassium, salts of alkaline earth metals, zinc, copper, ammonium salts, salts of basic amino acids, and salts of amines such as triethanolamine. The salts are preferably selected from alkali metal salts, alkaline earth metal salts, amine salts, zinc, and copper, and more preferably sodium, potassium, triethanolamine salts, zinc, and copper. Among these, a combination with one or more selected from gluconic acid, citric acid, glutamic acid, succinic acid, malic acid, salicylic acid, glycolic acid, phytic acid, tartaric acid, lactic acid, and glycyrrhetinic acid is more preferable.
上記糖類としては、例えば、例えば単糖類、二糖類、具体的にはグルコース、マルトース、トレハロース、スクロース、シクロデキストリン、キシリトール、ソルビトール、マンニトール等が挙げられる。 Examples of the above sugars include monosaccharides and disaccharides, specifically glucose, maltose, trehalose, sucrose, cyclodextrin, xylitol, sorbitol, mannitol, etc.
上記保湿成分としては、例えば、ジグリセリントレハロース、グリコシルトレハロース、トレハロース;ヒアルロン酸、アセチルヒアルロン酸、低分子ヒアルロン酸等のヒアルロン酸類又はその塩(ナトリウム、カリウム、亜鉛等の塩)又はその誘導体、ヘパリン類似物質、コンドロイチン硫酸ナトリウム等のムコ多糖類;MPCポリマー;コラーゲン、エラスチン、ケラチン、キチン、キトサン等とそれらの加水分解物;グリシン、アスパラギン酸、アルギニン等のアミノ酸;乳酸ナトリウム、尿素、ピロリドンカルボン酸ナトリウム等の天然保湿因子;セラミド、グルコシルセラミド、コレステロール、フィトステロール、コレステロール誘導体、フィトステロール誘導体、リン脂質等の脂質;カミツレエキス、ハマメリスエキス、チャエキス、シソエキス、グレープフルーツエキス等の植物抽出エキス;グリセリン、PPG-17ブテス-17、PPG-25ソルビトール、ポリオキシアルキレンアルキルグルコシド、PEG/PPG/ポリブチレングリコール-8/5/3グリセリンなどの多価アルコールまたはその誘導体;ソルビトール、キシリトール、エリスリトール、マルトース・ショ糖縮合物(グルコオリゴ糖)、加水分解キシラン(キシロオリゴ糖)などの糖アルコール;ヒドロキシエチルウレア等が挙げられる。中でもヒアルロン酸、低分子ヒアルロン酸、ヒアルロン酸ナトリウム、アセチルヒアルロン酸ナトリウム、ヒアルロン酸亜鉛、乳酸ナトリウム、ヘパリン類似物質、尿素、ピロリドンカルボン酸ナトリウム、トリメチルグリシン、MPCポリマー、加水分解コラーゲン、加水分解エラスチン、コラーゲン、セラミド、水素添加レシチンリン脂質、カミツレエキス、グレープフルーツエキス、多価アルコール、ポリオキシプロピレンメチルグルコシド、ヒドロキシエチルウレアから選ばれる1種又は2種以上との組み合わせがより好ましい。Examples of the moisturizing components include diglycerol trehalose, glycosyl trehalose, trehalose; hyaluronic acids such as hyaluronic acid, acetylated hyaluronic acid, and low molecular weight hyaluronic acid, or their salts (salts of sodium, potassium, zinc, etc.) or their derivatives, heparinoids, mucopolysaccharides such as sodium chondroitin sulfate, MPC polymers, collagen, elastin, keratin, chitin, chitosan, and the like, and their hydrolysates; amino acids such as glycine, aspartic acid, and arginine; natural moisturizing factors such as sodium lactate, urea, and sodium pyrrolidone carboxylate; ceramide, glucosylceramide, cholesterol, phytosulfate, etc. lipids such as sterol, cholesterol derivatives, phytosterol derivatives, and phospholipids; plant extracts such as chamomile extract, hamamelis extract, tea extract, perilla extract, and grapefruit extract; polyhydric alcohols or derivatives thereof such as glycerin, PPG-17 buteth-17, PPG-25 sorbitol, polyoxyalkylene alkyl glucoside, PEG/PPG/polybutylene glycol-8/5/3 glycerin; sugar alcohols such as sorbitol, xylitol, erythritol, maltose-sucrose condensates (glucooligosaccharides), and hydrolyzed xylan (xylooligosaccharides); and hydroxyethyl urea. Among these, a combination with one or more selected from hyaluronic acid, low molecular weight hyaluronic acid, sodium hyaluronate, sodium acetylated hyaluronate, zinc hyaluronate, sodium lactate, heparinoids, urea, sodium pyrrolidone carboxylate, trimethylglycine, MPC polymer, hydrolyzed collagen, hydrolyzed elastin, collagen, ceramide, hydrogenated lecithin phospholipid, chamomile extract, grapefruit extract, polyhydric alcohol, polyoxypropylene methylglucoside, and hydroxyethyl urea is more preferred.
上記多価アルコールとしては、炭素数2~10のものが好ましく、例えば、グリセリン、ジグリセリン、トリグリセリン、プロピレングリコール、ジプロピレングリコール、1,3-ブタンジオール、エチレングリコール、ジエチレングリコール、イソプレングリコール、1、3-ブチレングリコール、ソルビトール、キシリトール、エリスリトール、マンニトール、ペンタンジオール、ヘキサンジオール、オクタンジオール、デカンジオール、ネオペンチルグリコール、1,3-プロパンジオール等が挙げられる。中でもグリセリン、ジグリセリン、プロピレングリコール、ジプロピレングリコール、1、3-ブチレングリコール、ソルビトール、ペンタンジオール、ヘキサンジオール、オクタンジオールから選ばれる1種又は2種以上との組み合わせがより好ましい。The polyhydric alcohol preferably has 2 to 10 carbon atoms, such as glycerin, diglycerin, triglycerin, propylene glycol, dipropylene glycol, 1,3-butanediol, ethylene glycol, diethylene glycol, isoprene glycol, 1,3-butylene glycol, sorbitol, xylitol, erythritol, mannitol, pentanediol, hexanediol, octanediol, decanediol, neopentyl glycol, 1,3-propanediol, etc. Among these, a combination with one or more selected from glycerin, diglycerin, propylene glycol, dipropylene glycol, 1,3-butylene glycol, sorbitol, pentanediol, hexanediol, and octanediol is more preferred.
上記スクラブ剤としては、例えば、アプリコット核粉末、アーモンド殻粉末、アンズ核粉末、塩化ナトリウム粒、オリーブ核粉末、海水乾燥物粒、キャンデリラワックス、くるみ殻粉末、さくらんぼ核粉末、サンゴ粉末、炭粉末、はしばみ殻粉末、ポリエチレン末、無水ケイ酸等が挙げられる。Examples of the scrubbing agents include apricot kernel powder, almond shell powder, apricot kernel powder, sodium chloride granules, olive kernel powder, seawater dried granules, candelilla wax, walnut shell powder, cherry kernel powder, coral powder, charcoal powder, hazel shell powder, polyethylene powder, and anhydrous silicic acid.
上記紫外線吸収成分としては、例えば、オクチルトリアゾン、ジメトキシベンジリデンジオキソイミダゾリジンプロピオン酸オクチル、パラメトキシケイ皮酸2-エチルヘキシル、フェニルベンズイミダゾールスルホン酸、ジエチルアミノヒドロキシベンゾイル安息香酸ヘキシルエステル、ビスエチルヘキシルオキシフェノールメトキシフェニルトリアジン、t-ブチルメトキシジベンゾイルメタン、パラアミノ安息香酸およびその誘導体、パラジメチルアミノ安息香酸オクチル、ジヒドロキシベンゾフェノン、メチレンビスベンゾトリアゾリルテトラメチルブチルフェノール等が挙げられる。中でもパラメトキシケイ皮酸2-エチルヘキシル、ジエチルアミノヒドロキシベンゾイル安息香酸ヘキシルエステル、オクチルトリアゾン、ビスエチルヘキシルオキシフェノールメトキシフェニルトリアジン、t-ブチルメトキシジベンゾイルメタン、メチレンビスベンゾトリアゾリルテトラメチルブチルフェノールから選ばれる1種又は2種以上との組み合わせがより好ましい。Examples of the ultraviolet absorbing component include octyl triazone, dimethoxybenzylidene dioxoimidazolidine octyl propionate, 2-ethylhexyl paramethoxycinnamate, phenylbenzimidazole sulfonic acid, diethylamino hydroxybenzoyl benzoic acid hexyl ester, bisethylhexyloxyphenol methoxyphenyl triazine, t-butyl methoxydibenzoylmethane, paraaminobenzoic acid and its derivatives, octyl paradimethylaminobenzoate, dihydroxybenzophenone, methylene bisbenzotriazolyl tetramethylbutylphenol, etc. Among them, a combination with one or more selected from 2-ethylhexyl paramethoxycinnamate, diethylamino hydroxybenzoyl benzoic acid hexyl ester, octyl triazone, bisethylhexyloxyphenol methoxyphenyl triazine, t-butyl methoxydibenzoylmethane, and methylene bisbenzotriazolyl tetramethylbutylphenol is more preferred.
上記紫外線散乱成分としては、例えば、含水ケイ酸、ケイ酸亜鉛、ケイ酸セリウム、ケイ酸チタン、酸化ジルコニウム、酸化セリウム、酸化チタン、酸化亜鉛、酸化鉄、無水ケイ酸等の無機化合物、これらの無機化合物を含水ケイ酸、水酸化アルミニウム、マイカやタルク等の無機粉体で被覆したり、ポリアミド、ポリエチレン、ポリエステル、ポリスチレン、ナイロン等の樹脂粉体に複合化したもの、さらにシリコーン油や脂肪酸アルミニウム塩等で処理したもの等が挙げられる。Examples of the UV scattering components include inorganic compounds such as hydrous silicic acid, zinc silicate, cerium silicate, titanium silicate, zirconium oxide, cerium oxide, titanium oxide, zinc oxide, iron oxide, and anhydrous silicic acid; these inorganic compounds are coated with inorganic powders such as hydrous silicic acid, aluminum hydroxide, mica, and talc; or are composited with resin powders such as polyamide, polyethylene, polyester, polystyrene, and nylon; and further, are treated with silicone oil, aluminum salts of fatty acids, etc.
上記収斂成分としては、例えば、エタノール、硫酸亜鉛、塩化アルミニウム、スルホ石炭酸亜鉛等の金属塩、タンニン酸等の有機酸、植物(例えば海藻、タイム、紅茶、ウーロン茶、緑茶、オトギリソウ、ハマメリス、ビワ、ボタンピ、ユキノシタ、ルイボス、レンゲソウ、アーティチョーク、カミツレ、ユーカリ、レモン、ローズマリー、ワレモコウなど)に由来する成分等が挙げられる。Examples of the astringent ingredients include metal salts such as ethanol, zinc sulfate, aluminum chloride, and zinc sulfocarbonate, organic acids such as tannic acid, and ingredients derived from plants (e.g., seaweed, thyme, black tea, oolong tea, green tea, Hypericum, witch hazel, loquat, peonies, saxifrage, rooibos, astragalus, artichoke, chamomile, eucalyptus, lemon, rosemary, and burnet).
上記ペプチド又はその誘導体としては、例えば、ケラチン分解ペプチド、加水分解ケラチン、コラーゲン、魚由来コラーゲン、アテロコラーゲン、サクシニル化アテロコラーゲン、ゼラチン、エラスチン、エラスチン分解ペプチド、コラーゲン分解ペプチド、加水分解コラーゲン、塩化ヒドロキシプロピルアンモニウム加水分解コラーゲン、エラスチン分解ペプチド、コンキオリン分解ペプチド、加水分解コンキオリン、シルク蛋白分解ペプチド、加水分解シルク、ラウロイル加水分解シルクナトリウム、大豆蛋白分解ペプチド、加水分解大豆蛋白、小麦蛋白、小麦蛋白分解ペプチド、加水分解小麦蛋白、カゼイン分解ペプチド、アシル化ペプチド(パルミトイルオリゴペプチド、パルミトイルペンタペプチド、パルミトイルテトラペプチド等)等が挙げられる。中でもケラチン分解ペプチド、加水分解ケラチン、魚由来コラーゲンエラスチン、エラスチン分解ペプチド、コラーゲン分解ペプチド、加水分解コラーゲン、エラスチン分解ペプチド、加水分解シルク、大豆蛋白分解ペプチド、加水分解大豆蛋白、から選ばれる1種又は2種以上との組み合わせがより好ましい。Examples of the above peptides or derivatives thereof include keratin hydrolysis peptides, hydrolyzed keratin, collagen, fish-derived collagen, atelocollagen, succinylated atelocollagen, gelatin, elastin, elastin hydrolysis peptides, collagen hydrolysis peptides, hydrolyzed collagen, hydroxypropylammonium chloride hydrolyzed collagen, elastin hydrolysis peptides, conchiolin hydrolysis peptides, hydrolyzed conchiolin, silk proteolysis peptides, hydrolyzed silk, sodium lauroyl hydrolyzed silk, soybean proteolysis peptides, hydrolyzed soybean protein, wheat protein, wheat proteolysis peptides, hydrolyzed wheat protein, casein hydrolysis peptides, acylated peptides (palmitoyl oligopeptide, palmitoyl pentapeptide, palmitoyl tetrapeptide, etc.). Among these, a combination with one or more selected from keratin hydrolysis peptides, hydrolyzed keratin, fish-derived collagen elastin, elastin hydrolysis peptides, collagen hydrolysis peptides, hydrolyzed collagen, elastin hydrolysis peptides, hydrolyzed silk, soybean proteolysis peptides, and hydrolyzed soybean protein is more preferred.
上記アミノ酸又はその誘導体としては、例えば、ベタイン(トリメチルグリシン)、プロリン、ヒドロキシプロリン、アルギニン、リジン、セリン、グリシン、アラニン、フェニルアラニン、β-アラニン、スレオニン、グルタミン酸、グルタミン、アスパラギン、アスパラギン酸、システイン、シスチン、メチオニン、ロイシン、イソロイシン、バリン、ヒスチジン、トレオニン、チロシン、タウリン、γ-アミノ酪酸、γ-アミノ-β-ヒドロキシ酪酸、カルニチン、カルノシン、クレアチン、イプシロンアミノカプロン酸、トリプトファン、オルニチン、N-ステアロイル-L-グルタミン酸ナトリウム、ジラウロイルグルタミン酸リシン及びその塩、ラウロイルグルタミン酸ジ(フィトステリル/オクチルドデシル)、ラウロイルグルタミン酸ジ(オクチルドデシル/フィトステリル/ベヘニル)等が挙げられる。またこれらアミノ酸又はその誘導体は、水和物等の溶媒和物であってもよく、更にd体、l体、dl体の何れであってもよい。中でもl体のアミノ酸又はその誘導体から選ばれる1種又は2種以上が好ましい。Examples of the above amino acids or derivatives thereof include betaine (trimethylglycine), proline, hydroxyproline, arginine, lysine, serine, glycine, alanine, phenylalanine, β-alanine, threonine, glutamic acid, glutamine, asparagine, aspartic acid, cysteine, cystine, methionine, leucine, isoleucine, valine, histidine, threonine, tyrosine, taurine, γ-aminobutyric acid, γ-amino-β-hydroxybutyric acid, carnitine, carnosine, creatine, epsilon aminocaproic acid, tryptophan, ornithine, sodium N-stearoyl-L-glutamate, lysine dilauroyl glutamate and its salts, di(phytosteryl/octyldodecyl) lauroyl glutamate, di(octyldodecyl/phytosteryl/behenyl) lauroyl glutamate, etc. These amino acids or derivatives thereof may be in the form of a solvate such as a hydrate, and may be in any of the d-, l-, and dl-forms. Of these, one or more amino acids or derivatives thereof in the l-form are preferred.
上記洗浄成分としては、例えば、ラウリン酸カリウム、ミリスチン酸カリウム、パルミチン酸カリウム又はステアリン酸カリウム等のアルカリ金属塩、アルカノールアミド塩又はアミノ酸塩等から選ばれる石けん類;ココイルグルタミン酸塩、ココイルメチルタウリンNa、ココイルメチルタウリンタウリン塩、ココイルグリシン塩、ステアロイルグルタミン酸塩、ミリストイルグルタミン酸塩等のアミノ酸系界面活性剤;ラウレス硫酸Na等のエーテル硫酸エステル塩;ラウリルエーテル酢酸Na等のエーテルカルボン酸塩;アルキルスルホコハク酸エステルNa等のスルホコハク酸エステル塩;ヤシ油脂肪酸モノエタノールアミド、ヤシ油脂肪酸ジエタノールアミド等の脂肪酸アルカノールアミド;ラウリルリン酸ナトリウム、ポリオキシエチレンラウリルエーテルリン酸ナトリウム等のモノアルキルリン酸エステル塩;ヤシ油脂肪酸アミドプロピルジメチルアミノ酢酸ベタイン、ラウリルジメチルアミノ酢酸ベタイン、2-アルキル-N-カルボキシメチル-N-ヒドロキシエチルイミダゾリニウムベタイン、ラウリルヒドロキシスルホベタイン及びラウロイルアミドエチルヒドロキシエチルカルボキシメチルベタインヒドロキシプロピルリン酸ナトリウム等のベタイン型両性界面活性剤;ラウリルアミノプロピオン酸ナトリウム等のアミノ酸型両性界面活性剤;モノラウリル酸ポリオキシエチレン(80)ソルビタン等のソルビタン系界面活性剤等が挙げられる。塩としては、例えば、硫酸、塩酸又はリン酸等の鉱酸の塩、マレイン酸等の有機酸の塩、ナトリウム又はカリウム等のアルカリ金属塩、アルカリ土類金属塩、亜鉛、銅、アンモニウム塩、塩基性アミノ酸塩、トリエタノールアミンのようなアミン塩等が挙げられる。好ましくは、アルカリ金属塩、アルカリ土類金属塩、アミン塩、亜鉛、銅から選ばれることが好ましく、ナトリウム、カリウム、トリエタノールアミン塩、亜鉛、銅がより好ましい。 The above-mentioned cleaning components include, for example, soaps selected from alkali metal salts such as potassium laurate, potassium myristate, potassium palmitate, and potassium stearate, alkanolamide salts, and amino acid salts; amino acid surfactants such as cocoyl glutamate, sodium cocoyl methyl taurate, sodium cocoyl methyl taurate taurate, cocoyl glycine salt, stearoyl glutamate, and myristoyl glutamate; ether sulfate ester salts such as sodium laureth sulfate; ether carboxylate salts such as sodium lauryl ether acetate; sulfosuccinate ester salts such as sodium alkyl sulfosuccinate; fatty acid alkanolamides such as coconut oil fatty acid monoethanolamide and coconut oil fatty acid diethanolamide. canolamide; monoalkyl phosphate salts such as sodium lauryl phosphate and sodium polyoxyethylene lauryl ether phosphate; betaine-type amphoteric surfactants such as coconut oil fatty acid amidopropyl dimethylaminoacetate betaine, lauryl dimethylaminoacetate betaine, 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine, lauryl hydroxysulfobetaine and lauroyl amidoethyl hydroxyethyl carboxymethyl betaine hydroxypropyl phosphate sodium; amino acid-type amphoteric surfactants such as sodium lauryl aminopropionate; sorbitan-based surfactants such as polyoxyethylene (80) sorbitan monolaurate, etc. Examples of the salt include salts of mineral acids such as sulfuric acid, hydrochloric acid, and phosphoric acid, salts of organic acids such as maleic acid, alkali metal salts such as sodium or potassium, alkaline earth metal salts, zinc, copper, ammonium salts, basic amino acid salts, and amine salts such as triethanolamine. Preferably, the salt is selected from alkali metal salts, alkaline earth metal salts, amine salts, zinc, and copper, and more preferably sodium, potassium, triethanolamine salt, zinc, and copper.
上記角質柔軟成分としては、例えば、ラノリン、乳酸、サリチル酸、グルコン酸、グリコール酸、クエン酸、リンゴ酸、フルーツ酸、フィチン酸、尿素、イオウ、酒石酸、フェルラ酸等が挙げられる。なかでも、乳酸、乳酸ナトリウム、グリコール酸、サリチル酸、フィチン酸、クエン酸が好ましい。Examples of the keratin softening ingredients include lanolin, lactic acid, salicylic acid, gluconic acid, glycolic acid, citric acid, malic acid, fruit acid, phytic acid, urea, sulfur, tartaric acid, ferulic acid, etc. Of these, lactic acid, sodium lactate, glycolic acid, salicylic acid, phytic acid, and citric acid are preferred.
上記細胞賦活化成分としては、例えば、植物(たとえば、ビルベリー、ダイズ、レモングラス、アロエベラ、クロレラ、ヒオウギ、ヨクイニン、カミツレ、ドクダミ、ホップ、ニンジンなど)に由来する成分;ローヤルゼリー、ローヤルゼリーエキス;ホエイ、ヨーグルトエキス、加水分解乳タンパク等の乳清由来エキス、酵母エキスなど)に由来する成分、γ-アミノ酪酸等のアミノ酸類;レチノール、チアミン、リボフラビン、塩酸ピリドキシン、パントテン酸、ピロロキノリンキノン類等のビタミン類;グリコール酸、乳酸等のα-ヒドロキシ酸類;タンニン、フラボノイド、サポニン、アラントイン、プラセンタ、プロテオグリカン、感光素301号等が挙げられる。Examples of the cell activation components include components derived from plants (e.g., bilberry, soybean, lemongrass, aloe vera, chlorella, bean berry, coix seed, chamomile, dokudami, hops, carrots, etc.); royal jelly, royal jelly extract; whey-derived extracts such as whey, yogurt extract, hydrolyzed milk protein, yeast extract, etc.); amino acids such as γ-aminobutyric acid; vitamins such as retinol, thiamine, riboflavin, pyridoxine hydrochloride, pantothenic acid, pyrroloquinoline quinones, etc.; α-hydroxy acids such as glycolic acid and lactic acid; tannin, flavonoids, saponin, allantoin, placenta, proteoglycan, photosensitizer No. 301, etc.
上記老化防止成分としては、例えば、加水分解大豆タンパク、レチノイド(レチノール及びその誘導体、レチノイン酸、レチナール、酢酸レチノール、パルミチン酸レチノール等)、パンガミン酸、カイネチン、ウルソール酸、ウコンエキス、スフィンゴシン誘導体、ケイ素、ケイ酸、N-メチル-L-セリン、メバロノラクトン、ペプチド類(カプロオイルテトラペプチド-3、オリゴペプチド-24など)、植物(アーティチョーク、イザヨイバラ、海藻、ビルベリー、シラカバ、セイヨウオオバコ、トウキ、オウゴン、オトギリソウ、コンフリー、ニーム、ノバラ、ヒオウギ、ヒメフウロ、ボダイジュ、ボタンピ)に由来する成分等が挙げられる。中でも、加水分解大豆タンパク、レチノール、酢酸レチノール、パルミチン酸レチノール、カプロオイルテトラペプチド-3、オリゴペプチド-24、アーティチョーク葉エキス、海藻エキス、ビルベリー葉エキス、コンフリー葉エキス、ニーム葉エキス、ヒメフウロエキスが好ましい。Examples of the anti-aging ingredients include hydrolyzed soy protein, retinoids (retinol and its derivatives, retinoic acid, retinal, retinol acetate, retinol palmitate, etc.), pangamic acid, kinetin, ursolic acid, turmeric extract, sphingosine derivatives, silicon, silicic acid, N-methyl-L-serine, mevalonolactone, peptides (caproyl tetrapeptide-3, oligopeptide-24, etc.), and ingredients derived from plants (artichoke, Rosa robur, seaweed, bilberry, white birch, plantain, Angelica acutiloba, Scutellaria baicalensis, Hypericum perforatum, comfrey, neem, wild rose, Belamcanda chinensis, Geranium globulus, Lily of the valley, Peony root). Among these, hydrolyzed soy protein, retinol, retinol acetate, retinol palmitate, caprooyl tetrapeptide-3, oligopeptide-24, artichoke leaf extract, seaweed extract, bilberry leaf extract, comfrey leaf extract, neem leaf extract, and Geranium globulus extract are preferred.
上記抗糖化成分としては、例えば、ブドレジャアキシラリス葉エキス、ウメ果実エキス、エーデルワイスエキス、イチョウエキス、サクラ葉エキス、ザクロエキス、セイヨウオオバコエキス、セイヨウサンザシエキス、シャクヤクエキス、ドクダミエキス、ビルベリー葉エキス、緑茶エキス、紅茶エキス、マロニエエキス、ローマカミツレエキス、ヨモギエキス等の植物エキス、月見草油、アムラーの果実、果汁又はそれらの抽出物、L-アルギニン、L-リジン、加水分解カゼイン、加水分解性タンニン、カルノシン等が挙げられる。 Examples of the anti-glycation ingredients include plant extracts such as Budreja axillaris leaf extract, plum fruit extract, edelweiss extract, ginkgo biloba extract, cherry leaf extract, pomegranate extract, plantain extract, hawthorn extract, peony extract, Houttuynia cordata extract, bilberry leaf extract, green tea extract, black tea extract, horse chestnut extract, Roman chamomile extract, and mugwort extract, evening primrose oil, amla fruit, fruit juice or extracts thereof, L-arginine, L-lysine, hydrolyzed casein, hydrolyzable tannin, and carnosine.
上記血行促進作用成分としては、植物(例えば、オタネニンジン、アシタバ、アルニカ、イチョウ、ウイキョウ、エンメイソウ、オランダカシ、カミツレ、ローマカミツレ、カロット、ゲンチアナ、ゴボウ、コメ、サンザシ、シイタケ、ショウガ、セイヨウサンザシ、セイヨウネズ、センキュウ、センブリ、タイム、チョウジ、チンピ、トウガラシ、トウキ、トウニン、トウヒ、ニンジン、ニンニク、ブッチャーブルーム、ブドウ、ボタン、マロニエ、メリッサ、ユズ、ヨクイニン、リョクチャ、ローズマリー、ローズヒップ、チンピ、トウキ、トウヒ、モモ、アンズ、クルミ、トウモロコシ等)に由来する成分;カフェイン、トウガラシチンキ、ガンマーオリザノール、カプサイシン、アセチルコリン、イクタモール、カンタリスチンキ、ガンマーオリザノール、セファランチン、トラゾリン、ニコチン酸トコフェロール、酢酸トコフェロール、グルコシルヘスペリジン等が挙げられる。 The blood circulation promoting ingredients include plants (e.g., ginseng, angelica, arnica, ginkgo, fennel, burdock, oak, chamomile, Roman chamomile, carrot, gentian, burdock, rice, hawthorn, shiitake mushroom, ginger, European hawthorn, European juniper, cnidium rhizome, Swertia japonica, thyme, clove, tangerine, chili pepper, angelica, peach kernel, spruce, carrot, garlic, butcher's broom, grape, peony, marshmallow, etc.) Examples of ingredients that may be included in the composition include those derived from Chinese quince, melissa, yuzu, coix seed, ryokucha, rosemary, rose hips, tangerine, angelica tree, spruce, peach, apricot, walnut, corn, etc.); caffeine, capsicum tincture, gamma oryzanol, capsaicin, acetylcholine, ichthammol, cantharides tincture, gamma oryzanol, cepharanthine, tolazoline, tocopherol nicotinate, tocopherol acetate, glucosyl hesperidin, etc.
上記美白成分としては、例えば、トコフェロール、トラネキサム酸、アスコルビン酸とその塩、アスコルビン酸誘導体等のビタミンC類(アスコルビン酸リン酸エステルナトリウム、アスコルビン酸リン酸エステルマグネシウム、テトラ2-ヘキシルデカン酸アスコルビル、2-O-エチルアスコルビン酸、3-O-エチルアスコルビン酸、アスコルビン酸グルコシドなど)、アルブチン、コウジ酸、プラセンタ、エラグ酸、ニコチン酸アミド、ハイドロキノン、4-メトキシサリチル酸カリウム塩、リノール酸及びその誘導体、バチルアルコール、植物(例えば、イリス(アイリス)、アーモンド、アロエ、アセロラ、ウーロン茶、エイジツ、オウゴン、オウレン、オトギリソウ、オドリコソウ、海藻、カッコン、クチナシ、クジン、クロレラ、コメ、コメハイガ、オリザノール、コメヌカ、サイシン、サンショウ、シソ、シャクヤク、センキュウ、ソウハクヒ、ダイズ、納豆、茶、トウキ、トウキンセンカ、ハマメリス、ベニバナ、ボタンピ、ヨクイニン、アセンヤク、キウイ、クロマメ、ゲンチアナ、ゲンジン、セージ、ダイコン、ツツジ、パセリ、ヒイラギ、ホップ、タイム、チョウジ、チンピ、カンゾウ、カミツレ、プルーン、シモツケソウ、ムラサキシキブ、ソウズク、グレーブフルーツ、トゲナシ、レモン、キウイ、マツ、ニーム、アーティチョーク、スギナ、オオバク、メマツヨイグサ、ビルベリー、ヒメフウロ、アッケシソウ、セイヨウシロヤナギ、ユキノシタ、ツボクサ、ローズマリー、ラベンダー、サンシュユ等)に由来する成分等が挙げられる。中でもアスコルビン酸、アスコルビン酸グルコシド、3-O-エチルアスコルビン酸、テトラ2-ヘキシルデカン酸アスコルビル、アルブチン、コウジ酸、プラセンタ、ニコチン酸アミドから選ばれる1種又は2種以上との組み合わせがより好ましい。 Examples of the whitening ingredients include tocopherol, tranexamic acid, ascorbic acid and its salts, vitamin C derivatives such as ascorbic acid derivatives (sodium ascorbic acid phosphate, magnesium ascorbic acid phosphate, ascorbyl tetra-2-hexyldecanoate, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, ascorbic acid glucoside, etc.), arbutin, kojic acid, placenta, ellagic acid, nicotinamide, hydroquinone, potassium 4-methoxysalicylic acid, linoleic acid and its derivatives, batyl alcohol, plants (e.g., iris, almond, aloe, acerola, oolong tea, star anise, Scutellaria baicalensis, Coptis chinensis, Hypericum perforatum, white lamiaceum, seaweed, pueraria lobata, gardenia, lily of the valley, Chlorella, rice, rice hyphae, oryzanol, rice bran, saussurea, pepper, perilla, peony, cnidium, soybean, natto, tea, angelica tree, calendula, hamamelis, safflower, peonies, coix seed, astragalus, kiwi, black beans, gentian, gentiana, sage, radish, azalea, parsley, holly, hops, thyme, clove, tangerine , licorice, chamomile, prune, meadowsweet, purple bark, sorrel, grapefruit, thorn pear, lemon, kiwi, pine, neem, artichoke, horsetail, Chinese bark, evening primrose, bilberry, gelatin, Salicornia herb, white willow, saxifrage, Centella asiatica, rosemary, lavender, Cornus officinalis, etc.) etc. Among them, a combination with one or more selected from ascorbic acid, ascorbic acid glucoside, 3-O-ethyl ascorbic acid, ascorbyl tetra-2-hexyldecanoate, arbutin, kojic acid, placenta, and nicotinamide is more preferred.
上記充血除去成分としては、例えば、α-アドレナリン作動薬、具体的にはエピネフリン、塩酸エピネフリン、塩酸エフェドリン、塩酸オキシメタゾリン、塩酸テトラヒドロゾリン、塩酸ナファゾリン、塩酸フェニレフリン、塩酸メチルエフェドリン、酒石酸水素エピネフリン、硝酸ナファゾリン等が挙げられる。なお、これらはd体、l体又はdl体のいずれでもよい。Examples of the congestion relief component include α-adrenergic agonists, specifically epinephrine, epinephrine hydrochloride, ephedrine hydrochloride, oxymetazoline hydrochloride, tetrahydrozoline hydrochloride, naphazoline hydrochloride, phenylephrine hydrochloride, methylephedrine hydrochloride, epinephrine hydrogen tartrate, naphazoline nitrate, etc. These may be in the d-, l- or dl-form.
上記眼筋調節薬成分としては、例えば、アセチルコリンと類似した活性中心を有するコリンエステラーゼ阻害剤、具体的にはメチル硫酸ネオスチグミン、トロピカミド、ヘレニエン硫酸アトロピン等が挙げられる。 Examples of the above-mentioned ocular muscle regulating drug components include cholinesterase inhibitors having an active center similar to that of acetylcholine, specifically neostigmine methylsulfate, tropicamide, atropine helenien sulfate, etc.
上記抗ヒスタミン薬成分又は抗アレルギー薬成分としては、例えば、アシタザノラスト、ジフェンヒドラミン又はその塩酸塩などの塩、マレイン酸クロルフェニラミン、フマル酸ケトチフェン、レボカバスチン又はその塩酸塩などの塩、アンレキサノクス、イブジラスト、タザノモグリク酸ナトリウム、ペミロラストカリウム等が挙げられる。 Examples of the above antihistamine or antiallergic drug components include azalanolast, diphenhydramine or a salt thereof such as its hydrochloride, chlorpheniramine maleate, ketotifen fumarate, levocabastine or a salt thereof such as its hydrochloride, amlexanox, ibudilast, sodium tazanomoglycate, and pemirolast potassium.
上記ポリフェノール類には、クルクミノイド、フラバノン、スチルペノイド、ポリメトキシフラボノイド類、フラボノール、キサントノイド、カルコン、リグノイド、フラバノール、イソフラボン等のフラボノイド系ポリフェノール類、フェノール酸系ポリフェノール類があげられる。中でもクルクミノイド、ヘスペリジン、レスベラトロール、ノビレチン、ルチン、ケルセチン、マンジフェリン、カルタミン、リグナン、カテキン、イソフラボン、アントシアニン、タンニン、カカオマスポリフェノール、クロロゲン酸が特に好ましい。The polyphenols include flavonoid polyphenols such as curcuminoids, flavanones, stilpenoids, polymethoxyflavonoids, flavonols, xanthonoids, chalcones, lignoids, flavanols, and isoflavones, and phenolic acid polyphenols. Among them, curcuminoids, hesperidin, resveratrol, nobiletin, rutin, quercetin, mangiferin, carthamin, lignans, catechins, isoflavones, anthocyanins, tannins, cocoa mass polyphenols, and chlorogenic acid are particularly preferred.
(pH)
本発明の上記各種組成物及び各種剤のpHは、通常pH2.0~9.0であり、pH3~8.5であることが好ましく、pH3.5~8.0であることがより好ましく、pH4.0~7.5であることがさらに好ましい。なお、このpHはpH調整剤の使用により調整することができる。
(pH)
The pH of the above-mentioned various compositions and various agents of the present invention is usually pH 2.0 to 9.0, preferably
(各種組成物及び各種剤の製造方法)
本発明の上記各種組成物及び各種剤の製造方法は特に制限されず、必須成分である本発明のデビルズクロー抽出物、必要に応じて配合される上記他の成分、各種組成物又は各種剤を製造するのに必要な基剤又は担体、添加剤等を適宜選択、配合して、常法により製造することができる。
(Methods of producing various compositions and agents)
The manufacturing method of the above-mentioned various compositions and various agents of the present invention is not particularly limited, and they can be manufactured by a conventional method by appropriately selecting and mixing the devil's claw extract of the present invention, which is an essential component, the above-mentioned other components that are mixed as necessary, and bases or carriers, additives, etc. necessary for producing the various compositions or various agents.
本発明の上記各種組成物及び各種剤は、その必須成分及び上記で説明した他の成分等を、化粧品、医薬品、医薬部外品、食品等に通常使用される基剤又は担体、及び必要に応じて、後述する添加剤と共に常法に従い混合して、必要に応じて乳化又は可溶化を行い、各種の製剤形態の外用組成物とすることができる。The above-mentioned various compositions and agents of the present invention can be prepared into topical compositions in various formulations by mixing the essential components and other components described above in accordance with conventional methods with bases or carriers commonly used in cosmetics, pharmaceuticals, quasi-drugs, foods, etc., and, if necessary, with additives described below, and emulsifying or solubilizing as necessary.
上記基剤又は担体としては、例えば、流動パラフィン、イソパラフィン、ハードファット、マイクロクリスタリンワックス、ポリブテン、ポリエチレン末、スクワラン、ワセリン、ゲル化炭化水素(プラスチベース等)、オゾケライト、α-オレフィンオリゴマー、軽質流動パラフィン等の炭化水素;メチルポリシロキサン、高重合メチルポリシロキサン、環状シリコーン、アルキル変性シリコーン、アミノ変性シリコーン、ポリエーテル変性シリコーン、ポリグリセリン変性シリコーン、シリコーン・アルキル鎖共変性ポリエーテル変性シリコーン、架橋型シリコーン、シリコーン・アルキル鎖共変性ポリグリセリン変性シリコーン、ポリエーテル変性分岐シリコーン、ポリグリセリン変性分岐シリコーン、アクリルシリコーン、フェニル変性シリコーン、シリコーンレジン等のシリコーン油;ヤシ油、オリーブ油、コメヌカ油、シアバター、アボガド油、アマニ油、ツバキ油、マカデミアナッツ油、トウモロコシ油、サフラワー油、キョウニン油、シナモン油、ブドウ種子油、ヒマワリ油、アーモンド油、サザンカ油、ナタネ油、ゴマ油、カカオ脂、硬化ヤシ油、パーム油、パーム核油、モクロウ核油、モクロウ、小麦胚芽油、米胚芽油、綿実油、大豆油、落花生油、茶実油、月見草油、ククイナッツ油、ヘーゼルナッツ油等の油脂;ホホバ油、ミウロウ、キャンデリラロウ、コメヌカロウ、綿ロウ、カルナウバロウ、ラノリンまたはラノリン誘導体等のロウ類;セタノール、セトステアリルアルコール、ステアリルアルコール、ベヘニルアルコール、オクチルドデカノール、イソステアリルアルコール、フィトステロール、コレステロール等の高級アルコール;ラウリン酸、ミリスチン酸、パルミチン酸、ステアリン酸、ベヘン酸、オレイン酸、リノール酸、イソステアリン酸、12-ヒドロキシステアリン酸等の高級脂肪酸;エチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース等のセルロース誘導体;ポリビニルピロリドン;カラギーナン;ポリビニルブチラート;ポリエチレングリコール;ジオキサン;ブチレングリコールアジピン酸ポリエステル;アジピン酸ジイソプロピル、ミリスチン酸イソプロピル、ミリスチン酸オクチルドデシル、パルミチン酸イソプロピル、パルミチン酸セチル、イソノナン酸イソノニル、テトラ2-エチルヘキサン酸ペンタエリスリット等のエステル類;デキストリン、マルトデキストリン等の多糖類;カルボキシビニルポリマー、アルキル変性カルボキシビニルポリマー等のビニル系高分子;エタノール、イソプロパノール等の低級アルコール;エチレングリコールモノメチルエーテル、エチレングリコールモノエチルエーテル、エチレングリコールモノプロピルエーテル、ジエチレングリコールモノメチルエーテル、ジエチレングリコールモノエチルエーテル、ジエチレングリコールモノプロピルエーテル、ジエチレングリコールモノブチルエーテル、プロピレングリコールモノエチルエーテル、プロピレングリコールモノプロピルエーテル、ジプロピレングリコールモノエチルエーテル、ジプロピレングリコールモノプロピルエーテル等のグリコールエーテル;水等が挙げられる。以上説明した基剤又は担体は、1種単独で用いてもよいし、2種以上を併用してもよい。またそれらの使用量は当業者に公知の範囲から適宜選択される。Examples of the base or carrier include liquid paraffin, isoparaffin, hard fat, microcrystalline wax, polybutene, polyethylene powder, squalane, petrolatum, gelling hydrocarbons (such as Plastibase), ozokerite, α-olefin oligomers, and hydrocarbons such as light liquid paraffin; methylpolysiloxane, highly polymerized methylpolysiloxane, cyclic silicone, alkyl-modified silicone, amino-modified silicone, polyether-modified silicone, polyglycerin-modified silicone, silicone/alkyl chain co-modified polyether-modified silicone, crosslinked silicone, silicone/alkyl chain co-modified polyglycerin-modified silicone, polyether-modified branched silicone, polyglycerin-modified branched silicone, acrylic silicone, phenyl-modified silicone oils such as silicone and silicone resin; oils and fats such as coconut oil, olive oil, rice bran oil, shea butter, avocado oil, linseed oil, camellia oil, macadamia nut oil, corn oil, safflower oil, apricot kernel oil, cinnamon oil, grape seed oil, sunflower oil, almond oil, camellia oil, rapeseed oil, sesame oil, cocoa butter, hardened coconut oil, palm oil, palm kernel oil, Japan wax kernel oil, Japan wax, wheat germ oil, rice germ oil, cottonseed oil, soybean oil, peanut oil, tea seed oil, evening primrose oil, kukui nut oil, and hazelnut oil; waxes such as jojoba oil, miu wax, candelilla wax, rice bran wax, cotton wax, carnauba wax, lanolin or lanolin derivatives; cetanol, cetostearyl alcohol, stearyl alcohol, behenyl alcohol, octyldodecanol, isopropyl alcohol, ethylhexyl ... Higher alcohols such as stearyl alcohol, phytosterol, and cholesterol; higher fatty acids such as lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, linoleic acid, isostearic acid, and 12-hydroxystearic acid; cellulose derivatives such as ethyl cellulose, hydroxypropyl cellulose, and hydroxypropyl methylcellulose; polyvinylpyrrolidone; carrageenan; polyvinyl butyrate; polyethylene glycol; dioxane; butylene glycol adipate polyester; esters such as diisopropyl adipate, isopropyl myristate, octyldodecyl myristate, isopropyl palmitate, cetyl palmitate, isononyl isononanoate, and pentaerythritol tetra 2-ethylhexanoate. Examples of the base or carrier include esters, polysaccharides such as dextrin and maltodextrin, vinyl polymers such as carboxyvinyl polymers and alkyl-modified carboxyvinyl polymers, lower alcohols such as ethanol and isopropanol, glycol ethers such as ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, ethylene glycol monopropyl ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, diethylene glycol monopropyl ether, diethylene glycol monobutyl ether, propylene glycol monoethyl ether, propylene glycol monopropyl ether, dipropylene glycol monoethyl ether, and dipropylene glycol monopropyl ether, and water. The base or carrier described above may be used alone or in combination of two or more. The amount of each of them to be used may be appropriately selected from the range known to those skilled in the art.
本発明の各種組成物及び各種剤には、本発明の効果を損なわない範囲で、化粧品、医薬品、医薬部外品、食品等に添加される公知の添加剤、例えば、界面活性剤、安定化剤、緩衝剤、等張化剤、酸化防止剤、着色剤、パール光沢付与剤、分散剤、キレート剤、pH調整剤、保存剤、増粘剤、刺激低減剤、賦形剤、潤沢剤、結合剤、崩壊剤、溶剤、油脂、乳化剤、分散剤、懸濁化剤、安定剤、増粘剤、甘味料、着色剤、香料、酸化防止剤、酸味剤、果汁などの食品添加剤等を添加することができる。これらの添加剤は、1種単独で用いてもよいし、2種以上を併用することもできる。The various compositions and agents of the present invention may contain known additives added to cosmetics, pharmaceuticals, quasi-drugs, foods, etc., within the scope of not impairing the effects of the present invention, such as surfactants, stabilizers, buffers, isotonicity agents, antioxidants, colorants, pearlescent agents, dispersants, chelating agents, pH adjusters, preservatives, thickeners, irritation reducers, excipients, lubricants, binders, disintegrants, solvents, oils and fats, emulsifiers, dispersants, suspending agents, stabilizers, thickeners, sweeteners, colorants, flavorings, antioxidants, acidulants, and food additives such as fruit juice. These additives may be used alone or in combination of two or more.
上記界面活性剤としては、非イオン性界面活性剤、陽イオン性界面活性剤、陰イオン性界面活性剤、両性界面活性剤等のいずれでもよく、例えば、ソルビタンモノイソステアレート、ソルビタンモノラウレート、ソルビタンモノパルミテート、ソルビタンモノステアレート、ペンタ-2-エチルヘキシル酸ジグリセロールソルビタン、テトラ-2-エチルヘキシル酸ジグリセロールソルビタン等のソルビタン脂肪酸エステル類;モノステアリン酸プロピレングリコール等のプロピレングリコール脂肪酸エステル類;ポリオキシエチレン硬化ヒマシ油40(HCO-40)、ポリオキシエチレン硬化ヒマシ油50(HCO-50)、ポリオキシエチレン硬化ヒマシ油60(HCO-60)、ポリオキシエチレン硬化ヒマシ油80等の硬化ヒマシ油誘導体;モノラウリル酸ポリオキシエチレン(20)ソルビタン(ポリソルベート20)、モノステアリン酸ポリオキシエチレン(20)ソルビタン(ポリソルベート60)、モノオレイン酸ポリオキシエチレン(20)ソルビタン(ポリソルベート80)、イソステアリン酸ポリオキシエチレン(20)ソルビタン等のポリオキシエチレンソルビタン脂肪酸エステル類;ポリオキシエチレンモノヤシ油脂肪酸グリセリル;グリセリンアルキルエーテル;アルキルグルコシド;ポリオキシエチレンセチルエーテル等のポリオキシアルキレンアルキルエーテル;ステアリルアミン、オレイルアミン等のアミン類;ポリオキシエチレン・メチルポリシロキサン共重合体、ラウリルPEG-9ポリジメチルシロキシエチルジメチコン、PEG-9ポリジメチルシロキシエチルジメチコン等のシリコーン系界面活性剤等が挙げられる。The surfactant may be any of nonionic surfactants, cationic surfactants, anionic surfactants, amphoteric surfactants, etc., and examples thereof include sorbitan fatty acid esters such as sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, diglycerol sorbitan penta-2-ethylhexyl acid, and diglycerol sorbitan tetra-2-ethylhexyl acid; propylene glycol fatty acid esters such as propylene glycol monostearate; hydrogenated castor oil derivatives such as polyoxyethylene hydrogenated castor oil 40 (HCO-40), polyoxyethylene hydrogenated castor oil 50 (HCO-50), polyoxyethylene hydrogenated castor oil 60 (HCO-60), and polyoxyethylene hydrogenated
上記安定化剤としては、例えば、ポリアクリル酸ナトリウム、ジブチルヒドロキシトルエン、ブチルヒドロキシアニソール、トロメタモール、ナトリウムホルムアルデヒドスルホキシレート(ロンガリット)、トコフェロール、ピロ亜硫酸ナトリウム、モノエタノールアミン、モノステアリン酸アルミニウム、モノステアリン酸グリセリン等が挙げられる。Examples of the stabilizers include sodium polyacrylate, dibutylhydroxytoluene, butylhydroxyanisole, trometamol, sodium formaldehyde sulfoxylate (Rongalit), tocopherol, sodium pyrosulfite, monoethanolamine, aluminum monostearate, and glycerin monostearate.
上記緩衝剤としては、例えば、クエン酸緩衝剤、酢酸緩衝剤、炭酸緩衝剤、ホウ酸緩衝剤、リン酸緩衝剤等が挙げられる。具体的には、クエン酸、クエン酸ナトリウム、酢酸、酢酸カリウム、酢酸ナトリウム、炭酸水素ナトリウム、炭酸ナトリウム、ホウ酸、ホウ砂、リン酸、リン酸水素二ナトリウム、リン酸二水素ナトリウム、リン酸二水素カリウム等が挙げられる。Examples of the buffering agent include citrate buffer, acetate buffer, carbonate buffer, borate buffer, phosphate buffer, etc. Specific examples include citric acid, sodium citrate, acetic acid, potassium acetate, sodium acetate, sodium bicarbonate, sodium carbonate, boric acid, borax, phosphoric acid, disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, etc.
上記等張化剤として、例えば、亜硫酸水素ナトリウム、亜硫酸ナトリウム、塩化カリウム、塩化カルシウム、塩化ナトリウム、塩化マグネシウム、酢酸カリウム、酢酸ナトリウム、炭酸水素ナトリウム、炭酸ナトリウム、チオ硫酸ナトリウム、硫酸マグネシウム、リン酸水素二ナトリウム、リン酸二水素ナトリウム、リン酸二水素カリウム、グリセリン、プロピレングリコール等が挙げられる。 Examples of the above-mentioned isotonicity agents include sodium bisulfite, sodium sulfite, potassium chloride, calcium chloride, sodium chloride, magnesium chloride, potassium acetate, sodium acetate, sodium bicarbonate, sodium carbonate, sodium thiosulfate, magnesium sulfate, disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, glycerin, propylene glycol, etc.
上記酸化防止剤としては、例えば、ジブチルヒドロキシトルエン、ブチルヒドロキシアニソール、ソルビン酸、亜硫酸ナトリウム、アスコルビン酸、アスコルビン酸ナトリウム、アスコルビン酸ステアリン酸エステル、アスコルビン酸ステアリン酸ナトリウム、アスコルビン酸パルミチン酸エステル、トコフェロール、酢酸トコフェロール、トコトリエノール、亜硫酸水素塩、次亜硫酸ナトリウム、二酸化硫黄、EDTAカルシウム二ナトリウム、エリソルビン酸、エリソルビン酸ナトリウム、L-システイン塩酸塩、コエンザイムQ10等のユビキノン類、セサミン等のリグナン、クルクミン、カプサイシン、ジンゲロール、レスベラトロール、アントシアニン、シアニジン、ビルベリーエキスおよびこれらの類縁体もしくは誘導体等が挙げられる。中でも、ジブチルヒドロキシトルエン、アスコルビン酸、アスコルビン酸パルミチン酸エステル、トコフェロール、酢酸トコフェロール、コエンザイムQ10、レスベラトロール、アントシアニン、セサミン、クルクミン、カプサイシン、ジンゲロール、ビルベリーエキスが好ましい。Examples of the antioxidants include dibutylhydroxytoluene, butylhydroxyanisole, sorbic acid, sodium sulfite, ascorbic acid, sodium ascorbate, ascorbyl stearate, sodium ascorbyl stearate, ascorbyl palmitate, tocopherol, tocopherol acetate, tocotrienol, hydrogen sulfite, sodium hyposulfite, sulfur dioxide, calcium disodium EDTA, erythorbic acid, sodium erythorbate, L-cysteine hydrochloride, ubiquinones such as coenzyme Q10, lignans such as sesamin, curcumin, capsaicin, gingerol, resveratrol, anthocyanin, cyanidin, bilberry extract, and analogs or derivatives thereof. Among these, dibutylhydroxytoluene, ascorbic acid, ascorbyl palmitate, tocopherol, tocopherol acetate, coenzyme Q10, resveratrol, anthocyanin, sesamin, curcumin, capsaicin, gingerol, and bilberry extract are preferred.
上記着色剤としては、例えば、無機顔料、天然色素等が挙げられる。 Examples of colorants include inorganic pigments, natural dyes, etc.
上記パール光沢付与剤としては、例えばジステアリン酸エチレングリコール、モノステアリン酸エチレングリコール、ジステアリン酸トリエチレングリコール等が挙げられる。Examples of the pearlescent luster imparting agents include ethylene glycol distearate, ethylene glycol monostearate, triethylene glycol distearate, etc.
上記分散剤としては、例えば、ピロリン酸ナトリウム、ヘキサメタリン酸ナトリウム、ポリビニルアルコール、ポリビニルピロリドン、メチルビニルエーテル/無水マレイン酸架橋コポリマー、有機酸等が挙げられる。 Examples of the dispersing agents include sodium pyrophosphate, sodium hexametaphosphate, polyvinyl alcohol, polyvinylpyrrolidone, methyl vinyl ether/maleic anhydride crosslinked copolymer, organic acids, etc.
上記キレート剤としては、例えば、EDTA・2ナトリウム塩、EDTA・カルシウム・2ナトリウム塩、アスコルビン酸等が挙げられる。 Examples of the above chelating agents include EDTA disodium salt, EDTA calcium disodium salt, ascorbic acid, etc.
上記pH調整剤としては、例えば無機酸(リン酸、塩酸、硫酸等)、有機酸(乳酸、乳酸ナトリウム、クエン酸、クエン酸ナトリウム、コハク酸、コハク酸ナトリウム、グルコン酸、リンゴ酸ナトリウム等)、炭酸カリウム、炭酸水素ナトリウム、二酸化炭素、無機塩基(水酸化カリウム、水酸化ナトリウム等)、有機塩基(トリエタノールアミン、ジイソプロパノールアミン、トリイソプロパノールアミン等)等が挙げられる。Examples of the pH adjusters include inorganic acids (phosphoric acid, hydrochloric acid, sulfuric acid, etc.), organic acids (lactic acid, sodium lactate, citric acid, sodium citrate, succinic acid, sodium succinate, gluconic acid, sodium malate, etc.), potassium carbonate, sodium bicarbonate, carbon dioxide, inorganic bases (potassium hydroxide, sodium hydroxide, etc.), organic bases (triethanolamine, diisopropanolamine, triisopropanolamine, etc.), etc.
上記保存剤としては、例えば、安息香酸、安息香酸ナトリウム、デヒドロ酢酸、デヒドロ酢酸ナトリウム、パラオキシ安息香酸イソブチル、パラオキシ安息香酸イソプロピル、パラオキシ安息香酸ブチル、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、パラオキシ安息香酸ベンジル、パラオキシ安息香酸メチル、フェノキシエタノール、クロロブタノール、ベンジルアルコール、フェネチルアルコール、ソルビン酸、チモール、イソプロピルメチルフェノール、カプリルヒドロキサム酸、メチルイソチアゾリン、ブチルカルバミン酸ヨウ化プロピニル、1,3-プロパンジオール、1,2-ペンタンジオール、1,2-ヘキサンジオール、1,2-オクタンジオール又はその塩等が挙げられる。Examples of the preservatives include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl parahydroxybenzoate, isopropyl parahydroxybenzoate, butyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, benzyl parahydroxybenzoate, methyl parahydroxybenzoate, phenoxyethanol, chlorobutanol, benzyl alcohol, phenethyl alcohol, sorbic acid, thymol, isopropylmethylphenol, caprylhydroxamic acid, methylisothiazoline, iodopropynyl butylcarbamate, 1,3-propanediol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, or salts thereof.
上記増粘剤としては、例えば、ポリビニルアルコール、ポリビニルピロリドン、カルボキシビニルポリマー等のビニル系増粘剤、メチルセルロース、エチルセルロース、ヒドロキシエチルセルロース、ヒドロキシメチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、カルボキシメチルセルロース、カルボキシエチルセルロース、疎水化ヒドロキシプロピルメチルセルロース等のセルロース系増粘剤、グアーガム、ペクチン、プルラン、ゼラチン、ローカストビーンガム、カラギーナン、寒天、グルコマンナン、カードラン、ジェランガム、スクレロチウムガム、キサンタンガム、アクリル酸メタクリル酸アルキル共重合体、ポリエチレングリコール、ベントナイト、アルギン酸、アルギン酸プロピレングリコール、マクロゴール、コンドロイチン硫酸ナトリウム、ヒアルロン酸、ヒアルロン酸ナトリウム、(アクリル酸ヒドロキシエチル/アクリロイルジメチルタウリンNa)コポリマー、(アクリロイルジメチルタウリンアンモニウム/ビニルピロリドン)コポリマー等が挙げられる。Examples of the thickening agents include vinyl thickening agents such as polyvinyl alcohol, polyvinylpyrrolidone, and carboxyvinyl polymers; cellulose thickening agents such as methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxymethylcellulose, carboxyethylcellulose, and hydrophobized hydroxypropylmethylcellulose; guar gum, pectin, pullulan, gelatin, locust bean gum, carrageenan, agar, glucomannan, curdlan, gellan gum, sclerotium gum, xanthan gum, acrylates/alkyl methacrylate copolymers, polyethylene glycol, bentonite, alginic acid, propylene glycol alginate, macrogol, sodium chondroitin sulfate, hyaluronic acid, sodium hyaluronate, hydroxyethyl acrylate/sodium acryloyldimethyltaurate copolymer, and ammonium acryloyldimethyltaurate/vinylpyrrolidone copolymer.
上記刺激低減剤としては、例えば、メチルセルロース、エチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロースなどのセルロース誘導体、ポリビニルピロリドン、ポリビニルアルコール、アクリル酸系高分子、ゼラチン、アラビアゴム、プルラン、アルファー化デンプン、カンテン、トラガント、アルギン酸ナトリウム、アルギン酸プロピレングリコールエステル、甘草エキス、2-メタクリロイルオキシエチルホスホリルコリン等が挙げられる。Examples of the above-mentioned irritation reducers include cellulose derivatives such as methylcellulose, ethylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose, polyvinylpyrrolidone, polyvinyl alcohol, acrylic acid polymers, gelatin, gum arabic, pullulan, pregelatinized starch, agar, tragacanth, sodium alginate, propylene glycol alginate, licorice extract, and 2-methacryloyloxyethyl phosphorylcholine.
上記賦形剤としては、乳糖、白糖、塩化ナトリウム、ブドウ糖、デンプン、炭酸カルシウム、カオリン、微結晶セルロース、硅酸等が挙げられる。 The above excipients include lactose, sucrose, sodium chloride, glucose, starch, calcium carbonate, kaolin, microcrystalline cellulose, silicic acid, etc.
上記結合剤としては、精製白糖、ブドウ糖、トレハロース、乳糖、マルトース、サッカリンナトリウム、アスパルテーム、アセスルファムカリウム、マルトデキストリン等の多糖、トウモロコシデンプン、バレイショデンプン、コムギデンプンおよびこれらのα化デンプン、マンニトール、ソルビトール、キシリトール、エリスリトール、スクラロース等の糖アルコール、結晶セルロース、メチルセルロース、エチルセルロース、ヒプロメロース、ヒドロキシプロピルセルロース、カルボキシメチルセルロース、カルボキシメチルセルロースナトリウム、カルボキシメチルセルロースカルシウム、カルメロースカルシウム、ヒプロメロースフタル酸エステル、セルロースアセテートフタレート等のセルロース系高分子、リン酸カルシウム、ポリビニルピロリドンがあげられる。中でも、結晶セルロース、バレイショデンプン、マルトデキストリンが好ましい。Examples of the binder include polysaccharides such as refined sucrose, glucose, trehalose, lactose, maltose, sodium saccharin, aspartame, potassium acesulfame, and maltodextrin, corn starch, potato starch, wheat starch, and pregelatinized starches thereof, sugar alcohols such as mannitol, sorbitol, xylitol, erythritol, and sucralose, cellulose polymers such as crystalline cellulose, methylcellulose, ethylcellulose, hypromellose, hydroxypropyl cellulose, carboxymethylcellulose, sodium carboxymethylcellulose, calcium carboxymethylcellulose, carmellose calcium, hypromellose phthalate, and cellulose acetate phthalate, calcium phosphate, and polyvinylpyrrolidone. Among these, crystalline cellulose, potato starch, and maltodextrin are preferred.
上記崩壊剤としては、例えばデンプン、低置換度ヒドロキシプロピルセルロース、カルボキシメチルセルロースカルシウム、クロスカルメロースナトリウム、ヒドロキシプロピルスターチ、部分アルファー化デンプン、アルギン酸ナトリウム、カンテン末、炭酸水素ナトリウム、炭酸カルシウム、ラウリル硫酸ナトリウム、ステアリン酸モノグリセリド、乳糖などが挙げられる。Examples of disintegrants include starch, low-substituted hydroxypropyl cellulose, carboxymethylcellulose calcium, croscarmellose sodium, hydroxypropyl starch, partially pregelatinized starch, sodium alginate, agar powder, sodium bicarbonate, calcium carbonate, sodium lauryl sulfate, monoglyceride stearate, and lactose.
上記滑沢剤としては、ステアリン酸、ステアリン酸マグネシウム、ステアリン酸カルシウム、ステアリン酸ポリオキシル、セタノール、タルク、硬化油、ショ糖脂肪酸エステル、ジメチルポリシロキサン、ミツロウ、サラシミツロウ、ホウ砂、ポリエチレングリコールなどが挙げられる。 Examples of the above lubricants include stearic acid, magnesium stearate, calcium stearate, polyoxyl stearate, cetearyl alcohol, talc, hydrogenated oil, sucrose fatty acid ester, dimethylpolysiloxane, beeswax, white beeswax, borax, polyethylene glycol, etc.
上記油脂としては、パーム油、パーム核油、ヤシ油、コーン油、ヒマワリ油、サフラワー油、落花生油、ココアバター、綿実油、大豆油、菜種油、米油、コメ胚芽油、シソ油、亜麻仁油などの天然植物油等、牛脂、乳脂、豚脂、カカオ脂、魚油、鯨油、バター、バターオイル等の動物油脂並びにこれらの硬化油、脂肪酸(中鎖脂肪酸を含む)のグリセリド(グリセリド、ジグリセリド、トリグリセリドなど)、ミツロウ等が挙げられる。中でも、ミツロウが好ましい。 Examples of the above-mentioned fats and oils include natural vegetable oils such as palm oil, palm kernel oil, coconut oil, corn oil, sunflower oil, safflower oil, peanut oil, cocoa butter, cottonseed oil, soybean oil, rapeseed oil, rice oil, rice germ oil, perilla oil, and linseed oil, animal fats and oils such as beef tallow, milk fat, lard, cacao butter, fish oil, whale oil, butter, and butter oil, as well as hardened oils of these, glycerides of fatty acids (including medium-chain fatty acids) (glycerides, diglycerides, triglycerides, etc.), and beeswax. Of these, beeswax is preferred.
上記乳化剤、分散剤、懸濁化剤、安定剤としては、ポリエチレングリコール、プロピレングリコール、グリセリン、ソルビトールのような多価アルコール;グリセリン脂肪酸エステル、ショ糖脂肪酸エステル、ポリグリセリン脂肪酸エステル等の合成乳化剤や、レシチン類、サポニン、植物ステロール類、乳脂肪球皮膜等の天然乳化剤;カルボキシメチルセルロースナトリウム、カオリン、キサンタンガム、メチルセルロース、トラガント等が挙げられる。Examples of the above emulsifiers, dispersants, suspending agents, and stabilizers include polyhydric alcohols such as polyethylene glycol, propylene glycol, glycerin, and sorbitol; synthetic emulsifiers such as glycerin fatty acid esters, sucrose fatty acid esters, and polyglycerin fatty acid esters; natural emulsifiers such as lecithins, saponin, plant sterols, and milk fat globule membranes; sodium carboxymethylcellulose, kaolin, xanthan gum, methylcellulose, and tragacanth.
上記甘味料としては、ショ糖、果糖、麦芽糖、トレハロース、甘草抽出物、サッカリン、サッカリンナトリウム、スクラロース、ステビア加工甘味料、ラカンカ抽出物、アスパルテーム、アセスルファムカリウム、エリスリトール、ソルビトール、キシリトール、マルチトール、還元水飴、還元麦芽糖水飴などが挙げられる。 Examples of the sweeteners include sucrose, fructose, maltose, trehalose, licorice extract, saccharin, saccharin sodium, sucralose, stevia processed sweetener, Monk fruit extract, aspartame, acesulfame potassium, erythritol, sorbitol, xylitol, maltitol, reduced starch syrup, and reduced maltose syrup.
上記酸味剤としては、アジピン酸、イタコン酸、クエン酸、クエン酸カリウム、グルコノデルタラクトン、グルコン酸、コハク酸、コハク酸ナトリウム、酢酸ナトリウム、酒石酸、酒石酸ナトリウム、二酸化炭素、乳酸、乳酸ナトリウム、氷酢酸、フィチン酸、フマル酸、フマル酸ナトリウム、リンゴ酸、リン酸などが挙げられる。 Examples of the acidulants include adipic acid, itaconic acid, citric acid, potassium citrate, glucono-delta-lactone, gluconic acid, succinic acid, sodium succinate, sodium acetate, tartaric acid, sodium tartrate, carbon dioxide, lactic acid, sodium lactate, glacial acetic acid, phytic acid, fumaric acid, sodium fumarate, malic acid, and phosphoric acid.
上記果汁としては、レモン果汁、オレンジ果汁、ベリー系果汁、リンゴ果汁、バナナ果汁などが挙げられる。 Examples of the above fruit juices include lemon juice, orange juice, berry juice, apple juice, banana juice, etc.
(製剤形態)
本発明の各種組成物及び各種剤の形態は特に限定されず、例えば、軟膏剤、液剤、懸濁剤、乳化剤(乳液及びクリーム)、ゲル剤、リニメント剤、ローション剤、貼付剤、ミスト剤、フォーム剤、エアゾール剤、スティック剤、パウダー、顆粒、錠剤(素錠、糖衣錠、口腔内速崩壊錠、チュアブル錠、発泡錠、トローチ剤、フィルムコーティング錠等を含む)、洗浄剤、石鹸、固形剤、カプセル剤、フィルム剤、製菓剤(飴、グミ剤、ヌガー剤等を含む)、シロップ剤、ドリンク剤、ジュース、清涼飲料、茶等の液状食品、ビスケット、タブレット、顆粒粉末、粉末、カプセル等の固形、ペースト、ゼリー、スープ、調味料、ドレッシング等の半流動状等が挙げられる。これらの製剤は、常法、例えば第17改正日本薬局方製剤総則に記載の方法等に従い製造することができる。
(Form of preparation)
The form of the various compositions and preparations of the present invention is not particularly limited, and examples thereof include ointments, liquids, suspensions, emulsions (milky lotions and creams), gels, liniments, lotions, patches, mists, foams, aerosols, sticks, powders, granules, tablets (including plain tablets, sugar-coated tablets, oral rapid disintegrating tablets, chewable tablets, effervescent tablets, troches, film-coated tablets, etc.), detergents, soaps, solids, capsules, films, confectionery (including candy, gummies, nougat, etc.), syrups, drinks, juices, soft drinks, tea, and other liquid foods, biscuits, tablets, granular powders, powders, capsules, and other solids, pastes, jellies, soups, seasonings, dressings, and other semi-liquids, etc. These preparations can be produced according to conventional methods, for example, the methods described in the General Provisions for Preparations of the Japanese Pharmacopoeia, 17th Edition.
以下、実施例により本発明をより詳細に説明するが、本発明はこれらにより何ら限定されるものではない。The present invention will now be described in more detail with reference to the following examples, but the present invention is not limited to these in any way.
[試験1]デビルズクロー抽出物の製造
本発明のデビルズクロー抽出物を、以下の製造方法により取得した。本製造方法は、デビルズクロー乾燥粉末のエタノール抽出工程、抽出物の精製及び粉末化工程、及び粉末の再溶解工程から構成される。まず、原材料となるデビルズクロー乾燥粉末に対し50%(w/w)エタノール水溶液によって加熱抽出を行い、抽出液を得た。得られた抽出液は活性炭処理後、ろ過を行い、カラム精製を実施した。上記カラム精製では疎水性樹脂カラムを用い、抽出液から疎水性成分を除去し、精製抽出液を得た。次にこの精製抽出液からスプレードライ法により乾燥粉末を得た(製造例1~4)。得られた乾燥粉末、或いは必要に応じて1,3-BG水溶液に溶解したものを以下の試験に用いた。
[Test 1] Production of Devil's Claw Extract The devil's claw extract of the present invention was obtained by the following production method. This production method is composed of an ethanol extraction step of the devil's claw dry powder, a purification and powderization step of the extract, and a redissolution step of the powder. First, the raw material devil's claw dry powder was heated and extracted with a 50% (w/w) ethanol aqueous solution to obtain an extract. The obtained extract was treated with activated carbon, filtered, and purified by column. In the column purification, a hydrophobic resin column was used to remove hydrophobic components from the extract to obtain a purified extract. Next, a dry powder was obtained from this purified extract by spray drying (Production Examples 1 to 4). The obtained dry powder, or one dissolved in a 1,3-BG aqueous solution as necessary, was used in the following tests.
[試験2]Harpagoside(ハルパゴシド)の定量
試験1で得られた本発明のデビルズクロー抽出物の乾燥粉末4ロット(実生産スケールで製造した(製造例1~4))及び従来品4種について、Harpagosideの定量を行った。具体的には、各サンプルを秤量し、精製水に溶解後、水系0.45μmフィルター(GLサイエンス)にてフィルター後、試験サンプルとした。Harpagosideの定量は、Harpagosideの標品(SIGMA社)の検量線に基づいて行った。分析はHPLC(Agilent HPLC 1200)を使用し、以下の条件にて実施した。結果を表1に示す。表中の「N.D.」は検出限界以下であったことを示す。
紫外線吸光光度計 288nm、
カラム:Inertsil ODS 2 (5um, 4.6mm*150mm)、
移動相:23%MeCN:77% MiliQ water、
カラム温度 40℃、
流速 1.0 mL/min、
分析周期 30min、
インジェクション 20 uL
[Test 2] Quantification of Harpagoside Harpagoside was quantified for the four lots of dry powder of the Devil's Claw extract of the present invention obtained in Test 1 (manufactured on a commercial scale (Production Examples 1 to 4)) and four conventional products. Specifically, each sample was weighed, dissolved in purified water, filtered through an aqueous 0.45 μm filter (GL Science), and used as a test sample. Harpagoside was quantified based on the calibration curve of a harpagoside standard (SIGMA). Analysis was performed using HPLC (Agilent HPLC 1200) under the following conditions. The results are shown in Table 1. "N.D." in the table indicates that the amount was below the detection limit.
UV spectrophotometer 288 nm,
Column: Inertsil ODS2 (5um, 4.6mm*150mm),
Mobile phase: 23% MeCN: 77% MiliQ water,
Column temperature: 40°C;
Flow rate 1.0 mL/min,
Analysis period: 30 min.
上記表1に示すとおり、従来品4種には、Harpagosideが1.0%を超える高濃度で含まれているのに対し、本発明品である4ロットは、0.048%、0.003%又は検出限界以下と、従来品に比べて極めて低い濃度であった。As shown in Table 1 above, the four conventional products contained high concentrations of harpagoside exceeding 1.0%, whereas the four lots of the product of the present invention contained extremely low concentrations compared to the conventional products, at 0.048%, 0.003%, or below the detection limit.
[試験3]ポリフェノールの定量
試験1で得られた本発明のデビルズクロー抽出物の乾燥粉末4ロット(実生産スケールで製造した(製造例1~4))及び従来品4種について、ポリフェノールの定量を行った。具体的には、各サンプルを0.2g秤量し、50%エタノールを添加後、超音波照射による抽出を30分間行ったのち100mLに定容した。遠心分離後、上清をフィルターでろ過し、測定用のサンプルを得た。サンプル1mLに2倍希釈のFolin-Ciocalteu試薬(メルク株式会社)0.5mL及び0.4mоl/Lの炭酸ナトリウム水溶液5mLを添加し、30℃で30分間放置した。遠心分離後の上清の吸光度測定を、紫外可視分光光度計(V-630:日本分光株式会社)を使用し、660nmの測定波長にて実施した。ポリフェノールの定量は、(+)-カテキン水和物の標品(東京化成工業株式会社)の検量線に基づいて行った。結果を表2に示す。
[Test 3] Quantification of polyphenols Quantification of polyphenols was performed for the four lots of dry powder of the devil's claw extract of the present invention obtained in Test 1 (produced on a commercial scale (Production Examples 1 to 4)) and four conventional products. Specifically, 0.2 g of each sample was weighed out, 50% ethanol was added, and extraction was performed by ultrasonic irradiation for 30 minutes, and then the volume was adjusted to 100 mL. After centrifugation, the supernatant was filtered through a filter to obtain a sample for measurement. 0.5 mL of 2-fold diluted Folin-Ciocalteu reagent (Merck Co., Ltd.) and 5 mL of 0.4 mol/L aqueous sodium carbonate solution were added to 1 mL of the sample, and the mixture was allowed to stand at 30° C. for 30 minutes. The absorbance of the supernatant after centrifugation was measured using a UV-visible spectrophotometer (V-630: JASCO Corporation) at a measurement wavelength of 660 nm. Quantification of polyphenols was performed based on the calibration curve of a standard (+)-catechin hydrate (Tokyo Chemical Industry Co., Ltd.). The results are shown in Table 2.
上記表2に示すとおり、従来品4種には、ポリフェノールは3.0%を超える高濃度で含まれているのに対し、本発明品である4ロットは、従来品に比べて極めて低い濃度であった。As shown in Table 2 above, the four conventional products contained polyphenols at high concentrations exceeding 3.0%, whereas the four lots of the product of the present invention contained extremely low concentrations compared to the conventional products.
[試験4]着色評価試験
試験1で得られた本発明のデビルズクロー抽出物の乾燥粉末4ロット(実生産スケールで製造したもの)及び従来品4種について、着色評価を行った。具体的には、吸光度計を用いて着色量の評価を行った。測定検体としては、試験例1で使用した乾燥粉末を用いた。具体的には、それぞれの乾燥粉末を100mg秤量し、20mL精製水に懸濁、溶解させた(0.5%)。分光光度計又は光電光度計UV-2450(島津製作所製)で400-500nmの吸光度を測定した。ブランクとしては精製水を用いた。結果を図1及び図2に示す。また、目視により、従来品4種のデビルズクロー抽出物の乾燥粉末の溶液は茶色~褐色を帯びているのに対して、本発明のデビルズクロー抽出物の乾燥粉末4ロットの溶液はほぼ無色であることが確認できた(図3)。
[Test 4] Coloring evaluation test Coloring evaluation was performed on the four lots of dry powder of the Devil's Claw extract of the present invention (manufactured on a commercial scale) obtained in
図1及び2に示すとおり、従来品4種のデビルズクロー抽出物の乾燥粉末の溶液は着色の度合いが高いのに対して、本発明のデビルズクロー抽出物の乾燥粉末4ロットの溶液は着色の度合いが顕著に低いことがわかった。目視による結果(図3)とも相関した。このように、本発明のデビルズクロー抽出物は製剤において、見た目を損なうことなく配合することが可能であり、製剤原料として優れていることが明らかとなった。 As shown in Figures 1 and 2, the solutions of the dry powders of the four conventional Devil's Claw extracts were highly colored, whereas the solutions of the four lots of dry powder of the Devil's Claw extract of the present invention were significantly less colored. This correlated with the visual results (Figure 3). Thus, it was revealed that the Devil's Claw extract of the present invention can be incorporated into formulations without impairing the appearance, making it an excellent pharmaceutical ingredient.
[試験5]着色変化評価試験
原料の熱安定性は、製品の品質を確保することにおいて重要である。また、製品の着色変化は品質の劣化を示す指標ともなり得る。そこで製品に配合するデビルズクロー抽出物の安定性を評価するため、高温条件で保管したデビルズクロー抽出物の着色変化量を確認した。具体的には、試験1で得られた本発明のデビルズクロー抽出物(製造例1~4)及び従来品4種について、それぞれの乾燥粉末を100mg秤量し、20mL精製水に懸濁、溶解させた(0.5%(w/v))。60℃に設定した恒温槽に1週間保存し、1週間経過後に取り出し、分光光度計又は光電光度計UV-2450(島津製作所製)で400-500nmの吸光度を測定し、面積値を算出した。ブランクとしては精製水を用いた。結果を図4に示す。
[Test 5] Color change evaluation test The thermal stability of raw materials is important in ensuring the quality of products. In addition, color change of a product can be an indicator of deterioration of quality. Therefore, in order to evaluate the stability of the devil's claw extract to be blended in a product, the color change of the devil's claw extract stored under high temperature conditions was confirmed. Specifically, 100 mg of dry powder of each of the devil's claw extracts of the present invention (production examples 1 to 4) obtained in
図4に示すとおり、本発明のデビルズクロー抽出物の水溶液(製造例1~4)は、従来品4種のデビルズクロー抽出物の水溶液と比較して着色変化量が少ないことがわかった。即ち本発明のデビルズクロー抽出物は保管時変色が進みにくいことから、原料としての保管期間を延ばすことが可能となるため、原料として優れていることが明らかになった。 As shown in Figure 4, the aqueous solutions of the devil's claw extract of the present invention (Production Examples 1 to 4) showed less color change than the aqueous solutions of the four conventional devil's claw extracts. In other words, it was revealed that the devil's claw extract of the present invention is excellent as a raw material because it is less susceptible to discoloration during storage and therefore can be stored for an extended period as a raw material.
[試験6]透過度評価試験
原料の水に対する溶解性は、製剤中での析出等の観点から、製品の品質を確保することにおいて重要である。そこで原料の水に対する溶解性を、原料を精製水に懸濁、溶解させたサンプル(5%(w/w))の透過率を用いて評価した。従来品4種のデビルズクロー抽出物の乾燥粉末及び本発明のデビルズクロー抽出物(製造例1~4)をそれぞれ精製水に懸濁、溶解させたサンプルは、透明又は半透明の外観を呈していた。透過率の測定は、第17改正日本薬局方[B]一般試験法 2.物理的試験法 分光学的測定法 2.24紫外可視吸光度測定法に記載の方法に準ずる方法により行った。なお、本明細書において、原料の溶解性については以下のように判断した。すなわち、原料の水溶液(或いは水懸濁液)が、紫外可視吸光度測定法により、分光光度計又は光電光度計UV-2450(島津製作所製)を用いて波長700nmの透過率として、水の透過率を100%としたときに、85~100%、好ましくは90~100%の範囲にある場合、透過率が高く、水に対する溶解性に優れる、と判断する。結果を図5に示す。
[Test 6] Transmittance Evaluation Test The solubility of raw materials in water is important in terms of ensuring the quality of the product from the viewpoint of precipitation in the formulation. Therefore, the solubility of raw materials in water was evaluated using the transmittance of a sample (5% (w/w)) in which the raw materials were suspended and dissolved in purified water. Samples in which the dried powders of the four conventional Devil's Claw extracts and the Devil's Claw extracts of the present invention (Production Examples 1 to 4) were suspended and dissolved in purified water respectively had a transparent or translucent appearance. The transmittance was measured by a method similar to that described in the 17th Revised Japanese Pharmacopoeia [B]
図5に示すとおり、従来品4種のデビルズクロー抽出物の水溶液は、本発明のデビルズクロー抽出物の水溶液と比較して、同じ濃度で比較した場合、透過率が非常に低いことが判明した。即ち、従来のデビルズクロー抽出物は水に溶解させた際、濁りや析出を引き起こすことが判明した。一方、本発明のデビルズクロー抽出物を水に溶解させても、濁りや析出等が起こらず、製品の品質低下を引き起こしにくいことが明らかになった。 As shown in Figure 5, the aqueous solutions of the four conventional devil's claw extracts were found to have a very low transmittance when compared at the same concentration to the aqueous solution of the devil's claw extract of the present invention. In other words, it was found that the conventional devil's claw extract caused turbidity and precipitation when dissolved in water. On the other hand, it was found that the devil's claw extract of the present invention did not cause turbidity or precipitation when dissolved in water, and was unlikely to cause a deterioration in product quality.
[試験7]臭い試験
臭いは製品の評価に大きな影響を与えるが、従来のデビルズクロー抽出物は水に溶解させた際に特有の臭いを放つことが知られていた。本発明のデビルズクロー抽出物の乾燥粉末4ロット(実生産スケールで製造したもの(製造例1~4))及び従来品4種について、臭い官能試験を実施した。具体的には、それぞれの乾燥粉末5.0gを95mLの精製水に懸濁、溶解した(5%(w/w))。各サンプルを10mLガラスバイアルに分注し、60℃で1週間保存後、それぞれの臭いを官能試験によって確認した。官能試験は、健常な20-30代の男女3名にて行った。被験者にアンケートを記入してもらい、精製水(左)と各サンプル(右)の比較により臭いを数値化した。その際の臭いの数値化は以下のように行った。各サンプルにおける被験者の数値を平均化した結果を図6に示す。
[Test 7] Odor Test Odor has a significant effect on the evaluation of a product, and it is known that conventional devil's claw extracts emit a unique odor when dissolved in water. An odor sensory test was conducted on four lots of dry powder of the devil's claw extract of the present invention (manufactured on a commercial scale (Production Examples 1 to 4)) and four conventional products. Specifically, 5.0 g of each dry powder was suspended and dissolved in 95 mL of purified water (5% (w/w)). Each sample was dispensed into a 10 mL glass vial and stored at 60°C for one week, after which the odor of each sample was confirmed by a sensory test. The sensory test was conducted on three healthy men and women in their 20s and 30s. The subjects were asked to fill out a questionnaire, and the odor was quantified by comparing purified water (left) with each sample (right). The odor was quantified as follows. The results of averaging the subjects' values for each sample are shown in FIG. 6.
左が非常に臭い:-3点
左が臭い:-2点
左が少し臭い:-1点
同じ:0点
右が少し臭い:1点
右が臭い:2点
右が非常に臭い:3点
Left smells very bad: -3 points Left smells bad: -2 points Left smells a little bad: -1 point Same: 0 points Right smells a little bad: 1 point Right smells bad: 2 points Right smells very bad: 3 points
図6に示すとおり、従来品4種のデビルズクロー抽出物のサンプルは、本発明のデビルズクロー抽出物のサンプルと比較して、臭いが強いことが判明した。本発明のデビルズクロー抽出物のサンプルは、ほぼ精製水に近い数値となり、臭いをほとんど有していないことがわかった。このように本発明のデビルズクロー抽出物は、従来品に比べて臭いが少ないことから、様々な種類の製品に配合することが可能であり、好ましい。As shown in Figure 6, the four conventional devil's claw extract samples were found to have a stronger odor than the devil's claw extract sample of the present invention. The devil's claw extract sample of the present invention had a value close to that of purified water, and was found to have almost no odor. As such, the devil's claw extract of the present invention has less odor than conventional products, and is therefore preferable as it can be incorporated into various types of products.
[試験8]メラニン合成酵素遺伝子発現解析
試験1で得られた本発明のデビルズクロー抽出物(製造例3)の美白における有効性を確認するために、メラノサイトにおけるメラニン合成酵素(3種のメラニン合成酵素;TYR、TYRP1、DCT)の発現に対する作用を遺伝子レベルで解析した。6well plateにNHEM(ヒト正常表皮メラノサイトAD)(KURABO,KM-4109)を1×105cells/2mL/wellで播種し、37℃、5%CO2条件下にて培養した。72時間後、培養液を除去し、本発明品が0.1%、0.5%、1.0%の濃度で含まれる培地を2mL加え、さらに培養を行った。一定時間培養した後、Buffer RLT(QIAGEN)用いてRNAを回収した。粗抽出されたRNAは、RNeasy Mini Kit(Qiagen)を用いてカラム精製を行った。NanoDrop 1000 Spectrophotometer(Thermo Fisher Scientific)を使用しtotal RNAの濃度を測定した。逆転写反応液を調製し、Applied Biosystems(商標) Thermal Cycler(Thermo Fisher Scientific)を用いて、RNAの逆転写反応を行った。Premix Ex TaqTMキット(TaKaRa)およびQuantStudio 7 Flex Real-Time PCR System(Thermo Fisher Scientific)を用いて、リアルタイムPCR反応を行った。PCR反応回数は最大50サイクルとした。遺伝子発現量は、リアルタイムPCRにより得られた一定の増幅産物量になるサイクル数(threshold cycle値:Ct値)から2^-ΔΔCT値を算出し、r18Sをそれぞれ内部標準遺伝子とし、コントロールの値を1.00とした時の相対値を用いて比較した。各遺伝子のPCRプライマーは、Thermo Fisher Scientific社より市販されている推奨プライマーを用いた。結果を図7~10に示す。
[Test 8] Melanin synthesis enzyme gene expression analysis In order to confirm the effectiveness of the devil's claw extract of the present invention (Production Example 3) obtained in
本発明のデビルズクロー抽出物によって、NHEMにおける3種のメラニン合成関連酵素の遺伝子発現が抑制された。また、抑制レベルが最も大きいDCTについて経時的に解析した結果、いずれのタイムポイントにおいても本発明のデビルズクロー抽出物のDCT発現抑制作用が確認された。以上のことから、本発明のデビルズクロー抽出物は、メラニン合成酵素の発現を抑制する美白素材になる可能性が示唆された。The devil's claw extract of the present invention suppressed gene expression of three melanin synthesis-related enzymes in NHEM. Furthermore, a time-course analysis of DCT, which had the greatest level of suppression, confirmed that the devil's claw extract of the present invention has an inhibitory effect on DCT expression at all time points. These findings suggest that the devil's claw extract of the present invention may be a skin-whitening material that suppresses the expression of melanin synthesis enzymes.
[試験9]コラーゲン産生試験
試験1の製法により得た本発明のデビルズクロー抽出物(製造例5)及び本発明のデビルズクロー抽出物が含む各成分(スタキオース、スクロース、ラフィノース)の、シワ・たるみにおける有効性を確認するために、正常ヒト皮膚線維芽細胞(NHDF)におけるコラーゲン産生に対する作用をELISAにより検討した。本発明のデビルズクロー抽出物(製造例5)又は上記各成分を添加した培地でNHDFを培養し、その培地中に産生されたコラーゲン前駆体量をHuman Pro-Collagen I alpha 1 DuoSet ELISA(R&D社製)にて測定し、コラーゲン産生量の指標として評価した。結果を図11~14に示す。
[Test 9] Collagen Production Test In order to confirm the effectiveness of the devil's claw extract of the present invention obtained by the method of Test 1 (Production Example 5) and each component contained in the devil's claw extract of the present invention (stachyose, sucrose, raffinose) in wrinkles and sagging, the effect on collagen production in normal human dermal fibroblasts (NHDF) was examined by ELISA. NHDF was cultured in a medium containing the devil's claw extract of the present invention (Production Example 5) or each of the above components, and the amount of collagen precursor produced in the medium was measured by Human
本発明のデビルズクロー抽出物(1%)によって、顕著なコラーゲン産生促進作用が確認された。また、本発明品レベルには及ばないが、いずれの有効成分(スタキオース、スクロース、ラフィノース)においても濃度依存的なコラーゲン産生促進作用が確認された。本発明のデビルズクロー抽出物(1%)で確認された効果は、これらの有効成分の効果が合わさって見られたものであることが示唆された。以上のことから、本発明のデビルズクロー抽出物はシワ・たるみに優れた効果を示す抗シワ、アンチエイジング素材になる可能性が示唆された。 A significant collagen production promoting effect was confirmed by the devil's claw extract (1%) of the present invention. In addition, although not at the level of the product of the present invention, a concentration-dependent collagen production promoting effect was confirmed for each of the active ingredients (stachyose, sucrose, raffinose). It is suggested that the effect confirmed by the devil's claw extract (1%) of the present invention is the combined effect of these active ingredients. From the above, it is suggested that the devil's claw extract of the present invention may be an anti-wrinkle, anti-aging material that is highly effective against wrinkles and sagging.
[試験10]エラスチン線維形成試験
試験1で得られた製造例3の本発明のデビルズクロー抽出物のシワ・たるみにおける有効性を確認するために、正常ヒト皮膚線維芽細胞(NHDF)によるエラスチン線維形成に対する作用を免疫染色にて検討した。本発明のデビルズクロー抽出物(製造例3)を添加した培地でNHDFを培養し、エラスチン線維形成を免疫染色にて評価した。結果を図15に示す。
[Test 10] Elastin fiber formation test In order to confirm the effectiveness of the devil's claw extract of the present invention of Production Example 3 obtained in
足場となる2%FBSの添加によりエラスチン線維形成が起こり、0.05%の濃度で本発明のデビルズクロー抽出物を添加した培地で培養することで、その線維形成がさらに促進されたことを確認した。以上のことから、本発明のデビルズクロー抽出物はシワ・たるみに効果を示す抗シワ、アンチエイジング素材になる可能性が示唆された。It was confirmed that the addition of 2% FBS as a scaffold caused elastin fiber formation, and that fiber formation was further promoted by culturing in a medium containing the devil's claw extract of the present invention at a concentration of 0.05%. From the above, it was suggested that the devil's claw extract of the present invention may be an anti-wrinkle and anti-aging material that is effective against wrinkles and sagging.
[試験11]ヒアルロン酸産生試験-1
ウサギ由来軟骨培養細胞(プライマリーセルより入手)を用いて、ヒアルロン酸産生試験において、外用剤および経口、食品素材としての試験1で得られた本発明品(製造例4)の有用性評価を行った。
[Test 11] Hyaluronic acid production test-1
Using rabbit-derived cartilage culture cells (obtained from Primary Cell), the usefulness of the product of the present invention (Production Example 4) obtained in
具体的には、ウサギ由来軟骨培養細胞を、1.5mL用マイクロチューブ中で三次元培養した。その際、培地には本発明品製造例3(最終濃度0.1、1、10mg/mL)添加分化培地および無添加分化培地を用いた。培地交換は5-7日ごとに行った。培養は18日間行い、回収日の1週間前に最終の培地交換を行った。培養液を採取し、培養液中に分泌されたヒアルロン酸量を酵素結合免疫測定法(Hyaluronan Quantikine ELISA Kit;R&D社製)で定量した。結果を図16に示す。Specifically, rabbit-derived chondrocytes were cultured three-dimensionally in 1.5 mL microtubes. The differentiation medium used was either the one containing Example 3 of the present invention (final concentrations 0.1, 1, and 10 mg/mL) or the one without the product. The medium was replaced every 5-7 days. The culture was continued for 18 days, with the final medium replacement being performed one week before the harvest date. The culture medium was collected, and the amount of hyaluronic acid secreted into the culture medium was quantified by enzyme-linked immunosorbent assay (Hyaluronan Quantikine ELISA Kit; manufactured by R&D). The results are shown in Figure 16.
図16に示すとおり、本発明品を10mg/mL添加することで軟骨細胞においてヒアルロン酸産生量が大幅に向上することが判明した。即ち、加齢に伴う関節の痛みの原因の一つにヒアルロン酸など関節成分の減少が挙げられるが、本発明品の摂取によって関節症を改善する効果が期待される。 As shown in Figure 16, it was found that the addition of 10 mg/mL of the product of the present invention significantly improved the amount of hyaluronic acid produced in chondrocytes. In other words, one of the causes of joint pain associated with aging is a decrease in joint components such as hyaluronic acid, and it is expected that the ingestion of the product of the present invention will have the effect of improving arthropathy.
[試験12]ヒアルロン酸産生試験-2
正常ヒト皮膚線維芽細胞(NHDF)(KURABOより入手)を用いて、ヒアルロン酸産生試験において、外用剤および経口、食品素材としての試験1で得られた本発明品(製造例4)の有用性評価を行った。
[Test 12] Hyaluronic acid production test-2
Using normal human dermal fibroblasts (NHDF) (obtained from KURABO), the usefulness of the product of the present invention obtained in Test 1 (Production Example 4) as an external agent, oral administration, and food material was evaluated in a hyaluronic acid production test.
具体的には、NHDFを本発明のデビルズクロー抽出物(製造例4)又は陽性対照のN-アセチルグルコサミン(Wako)を添加した培地で48時間培養し、培地中に産生されたヒアルロン酸量をHyaluronan Quantikine ELISA Kit(R&D社製)にて測定した。また、培地採取後、Hoechst33342(DOJINDO)を添加した培地に入れ替え、37℃,5%CO2条件下にて30分間培養し、染色された核をカウントして細胞生存率の指標とした。ヒアルロン酸量を細胞生存率で除すことで、細胞当たりのヒアルロン酸産生量を評価した。結果を図17に示す。 Specifically, NHDF was cultured for 48 hours in a medium containing the devil's claw extract of the present invention (Production Example 4) or the positive control N-acetylglucosamine (Wako), and the amount of hyaluronic acid produced in the medium was measured using a Hyaluronan Quantikine ELISA Kit (manufactured by R&D Co., Ltd.). After collection of the medium, the medium was replaced with a medium containing Hoechst33342 (DOJINDO), and cultured for 30 minutes under conditions of 37°C and 5% CO2 , and the stained nuclei were counted to be used as an index of cell viability. The amount of hyaluronic acid produced per cell was evaluated by dividing the amount of hyaluronic acid by the cell viability. The results are shown in FIG. 17.
図17に示すとおり、本発明のデビルズクロー抽出物(0.5%)を添加することによって、正常ヒト皮膚線維芽細胞においてヒアルロン酸産生量が大幅に向上することが判明した。即ち、加齢に伴う皮膚のシワ、たるみ等の原因の一つにヒアルロン酸の減少が挙げられるが、本発明品の摂取によってこれらの症状を改善する効果が期待され、シワ・たるみに効果を示す抗シワ、アンチエイジング素材になる可能性が示唆された。 As shown in Figure 17, it was found that the addition of the devil's claw extract (0.5%) of the present invention significantly increased the amount of hyaluronic acid produced in normal human skin fibroblasts. In other words, one of the causes of wrinkles and sagging skin that accompany aging is a decrease in hyaluronic acid, but it is expected that the ingestion of the product of the present invention will improve these symptoms, suggesting the possibility that it could become an anti-wrinkle, anti-aging material that is effective against wrinkles and sagging skin.
[試験13]Gobi Kosa Dust(GKD)誘発炎症試験-1
正常ヒト表皮細胞(NHEK)(KURABOより入手)を用いて、大気汚染の原因物質であるGKDが誘発する炎症に対する、外用剤および経口、食品素材としての試験1で得られた本発明品(製造例4)の有用性評価を行った。
[Test 13] Gobi Kosa Dust (GKD)-induced inflammation test-1
Using normal human epidermal cells (NHEK) (obtained from KURABO), the usefulness of the product of the present invention obtained in Test 1 (Production Example 4) as an external agent, oral administration, and food ingredient against inflammation induced by GKD, a causative agent of air pollution, was evaluated.
具体的には、NHEKを本発明のデビルズクロー抽出物(製造例4)およびGKDを添加した培地で24時間培養し、NHEKのRNAを回収し、IL-8およびIL-6遺伝子発現量をリアルタイムPCR反応にて解析した。Specifically, NHEKs were cultured for 24 hours in a medium containing the devil's claw extract of the present invention (Example 4) and GKD, NHEK RNA was collected, and the expression levels of IL-8 and IL-6 genes were analyzed by real-time PCR reaction.
図18に示すとおり、本発明のデビルズクロー抽出物(1.0%および1.5%)を添加することによって、正常ヒト表皮細胞においてGKDが誘発する炎症性サイトカインであるIL-8およびIL-6の発現を有意に抑制させることが判明した。即ち、本発明品の摂取、または塗布、洗浄によってGKD曝露に伴う皮膚の炎症等を改善する効果が期待された。 As shown in Figure 18, it was found that the addition of the devil's claw extract of the present invention (1.0% and 1.5%) significantly suppressed the expression of IL-8 and IL-6, which are inflammatory cytokines induced by GKD, in normal human epidermal cells. In other words, it was expected that the ingestion, application, or washing of the product of the present invention would have the effect of improving skin inflammation and other conditions associated with GKD exposure.
[試験14]Gobi Kosa Dust(GKD)誘発炎症試験-2
ヒト角膜上皮細胞(HCET)(RIKEN BRCより入手)を用いて、大気汚染の原因物質であるGKDが誘発する炎症に対する、外用剤(皮膚化粧品、洗浄剤等含む)、眼科用製剤(点眼剤、洗眼剤、眼軟膏等)、および経口、食品素材としての試験1で得られた本発明品(製造例4)の有用性評価を行った。
[Test 14] Gobi Kosa Dust (GKD)-induced inflammation test-2
Using human corneal epithelial cells (HCET) (obtained from RIKEN BRC), the usefulness of the product of the present invention obtained in Test 1 (Production Example 4) as a topical agent (including skin cosmetics, detergents, etc.), ophthalmic preparation (eye drops, eye washes, eye ointments, etc.), and oral and food ingredients against inflammation induced by GKD, a causative substance of air pollution, was evaluated.
具体的には、HCETを本発明のデビルズクロー抽出物(製造例4)を添加した培地で1時間培養し、その後GKDを添加した。24時間培養した後、HCETのRNAを回収し、IL-1β、IL-8およびIL-6の遺伝子発現量をリアルタイムPCR反応にて解析した。Specifically, HCET was cultured for 1 hour in a medium containing the devil's claw extract of the present invention (Production Example 4), and then GKD was added. After culturing for 24 hours, HCET RNA was collected and the gene expression levels of IL-1β, IL-8, and IL-6 were analyzed by real-time PCR reaction.
図19に示すとおり、本発明のデビルズクロー抽出物(0.5%)を添加することによって、ヒト角膜上皮細胞においてGKDが誘発する炎症性サイトカインであるIL-1β、IL-8およびIL-6の発現を有意に抑制させることが判明した。即ち、本発明品の摂取、または本発明品による洗浄・塗布によってGKD曝露に伴う眼の炎症等を改善する効果が期待された。 As shown in Figure 19, it was found that the addition of the devil's claw extract (0.5%) of the present invention significantly suppressed the expression of IL-1β, IL-8, and IL-6, which are inflammatory cytokines induced by GKD in human corneal epithelial cells. In other words, it was expected that the ingestion of the product of the present invention or the washing and application of the product of the present invention would have the effect of improving ocular inflammation and the like associated with GKD exposure.
以下に、本発明のデビルズクロー抽出物を含有する外用組成物(化粧品、医薬部外品、医薬品)、経口用組成物(医薬品、サプリメント、ドリンク、一般食品等)の製剤処方例を示す。 Below are examples of formulations for topical compositions (cosmetics, quasi-drugs, medicines) and oral compositions (medicines, supplements, drinks, general foods, etc.) containing the devil's claw extract of the present invention.
[外用組成物]
下記表中の数値は各成分の濃度(重量%)を示している。
[External Composition]
The values in the table below indicate the concentration (wt %) of each component.
[ソフトカプセル]
下記表中の数値はソフトカプセルの各処方例における各成分の一日摂取量(mg)を示している。
The values in the table below indicate the daily intake (mg) of each ingredient in each soft capsule formulation example.
[錠剤]
下記表中の数値は錠剤の各処方例における各成分の一日摂取量(mg)を示している。
[tablet]
The values in the table below indicate the daily intake (mg) of each ingredient in each tablet formulation example.
[顆粒剤]
下記表中の数値は顆粒剤の処方例における各成分の一日摂取量(mg)を示している。
[Granules]
The values in the table below indicate the daily intake (mg) of each ingredient in the granule formulation example.
[ドリンク]
下記表中の数値はドリンクの処方例における各成分の一日摂取量(mg)を示している。
[Drink]
The numbers in the table below show the daily intake (mg) of each ingredient in the drink formulation example.
[ゼリー]
下記表中の数値はゼリーの各処方例における各成分の一日摂取量(mg)を示している。
[jelly]
The numbers in the table below indicate the daily intake (mg) of each component in each jelly formulation example.
[グミ]
下記表中の数値はグミの各処方例における各成分の一日摂取量(mg)を示している。
[Gummy]
The numbers in the table below indicate the daily intake (mg) of each ingredient in each gummy formulation.
[外用組成物]
下記表には、外用組成物の処方例(処方例20~33)を示す。各表中の数値は各成分の濃度(重量%)を示している。
[External Composition]
The following tables show examples of formulations of topical compositions (Formulation Examples 20 to 33). The values in each table indicate the concentration (wt%) of each component.
下記表10(表10-1及び10-2)は、アンチポリューション作用を有する外用剤の処方例である。Table 10 below (Tables 10-1 and 10-2) is an example of a prescription for an external preparation with anti-pollution properties.
下記表11は、洗浄剤(泡吐出タイプ)の処方例である。 Table 11 below is an example of a formulation for a cleaning agent (foam type).
下記表12は、シャンプーの処方例(処方例30)である。 Table 12 below is an example of a shampoo formulation (Formulation Example 30).
下記表13は、クレンジングの処方例(処方例31)である。 Table 13 below is an example of a cleansing formulation (Formulation Example 31).
下記表14は、洗浄剤(クリームタイプ)の処方例(処方例32)である。 Table 14 below is an example of a formulation for a cleanser (cream type) (Formulation Example 32).
下記表15は、洗眼剤の処方例(処方例33)である。 Table 15 below is an example of an eyewash formulation (Formulation Example 33).
本発明のデビルズクロー抽出物は、従来のデビルズクロー抽出物から、有効成分として知られていたハルパゴシド等の疎水性の物質を除去したものであり、ハルパゴシドの含有量が1.0重量%以下と顕著に抑えられた新規のエキスである。従来のデビルズクロー抽出物と異なり、独特の着色や臭い、苦味が生じないことから安定性にも優れ、溶解性も高いことから、様々な製品に配合し易いという利点がある。また、この本発明のデビルズクロー抽出物は、皮膚におけるメラニン合成酵素遺伝子発現抑制作用、コラーゲン産生促進作用、エラスチン線維形成促進作用、ヒアルロン酸産生促進作用、大気汚染物質により誘発される炎症性物質の産生抑制効果等を有し、美白、抗シワ、アンチエイジング、関節症改善効果、抗炎症効果(アンチポリューション)も期待できる。さらに、ハルパゴシド等のイリドイド類は苦味を有しかつ様々な薬理効果を有することが知られており、従来のデビルズクロー抽出物は、投与経路、適用部位、適用対象によっては、不都合が生じることがあった。しかし、本発明のデビルズクロー抽出物はイリドイド類の含有量が顕著に抑えられているため、上記の制限が不要であり、安全性にも優れている。以上のことから、本発明のデビルズクロー抽出物は、化粧品、医薬品、医薬部外品、食品(機能性食品、サプリメント、ドリンク剤等)等として、また、その形態については外用組成物、経口用組成物(食品組成物を含む)、眼科用組成物等として好適に使用することができる。The devil's claw extract of the present invention is a novel extract obtained by removing hydrophobic substances such as harpagoside, which was known as an active ingredient, from the conventional devil's claw extract, and the content of harpagoside is significantly reduced to 1.0% by weight or less. Unlike conventional devil's claw extracts, it has excellent stability and high solubility because it does not produce unique coloring, odor, or bitterness, and has the advantage of being easily blended into various products. In addition, the devil's claw extract of the present invention has an effect of suppressing melanin synthesis enzyme gene expression in the skin, an effect of promoting collagen production, an effect of promoting elastin fiber formation, an effect of promoting hyaluronic acid production, an effect of suppressing the production of inflammatory substances induced by air pollutants, etc., and can be expected to have whitening, anti-wrinkle, anti-aging, arthropathy improvement effects, and anti-inflammatory effects (anti-pollution). Furthermore, iridoids such as harpagoside are known to have a bitter taste and various pharmacological effects, and conventional devil's claw extracts may cause inconvenience depending on the administration route, application site, and application target. However, the devil's claw extract of the present invention has a significantly reduced content of iridoids, so the above restrictions are unnecessary and it is also safe. For these reasons, the devil's claw extract of the present invention can be suitably used as cosmetics, medicines, quasi-drugs, foods (functional foods, supplements, drinks, etc.), and in the form of an external composition, an oral composition (including food compositions), an ophthalmic composition, etc.
Claims (8)
を含む製造方法によって取得され、乾燥重量当たりのハルパゴシド含有量が1.0重量%以下である、デビルズクロー抽出物
を含有する外用組成物。 A step of extracting the dried devil's claw powder with a 30% to 70% (w/w) aqueous ethanol solution by heating to obtain an extract, and a step of removing hydrophobic components from the extract using a hydrophobic resin column.
and a devil's claw extract having a harpagoside content of 1.0% by weight or less per dry weight.
A topical composition comprising:
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JP2018184174 | 2018-09-28 | ||
JP2018184174 | 2018-09-28 | ||
PCT/JP2019/016339 WO2019230233A1 (en) | 2018-05-28 | 2019-04-16 | Devil's-claw extract and variety of compositions containing same, and production method for devil's-claw extract |
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CN113615862B (en) * | 2021-08-02 | 2023-03-17 | 深圳市真味生物科技有限公司 | Aromatic plant electronic atomized liquid and preparation method thereof |
CN116850117B (en) * | 2023-05-26 | 2024-02-09 | 天地慈(东莞)生物科技有限公司 | Whitening and brightening composition and preparation method thereof |
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JP2001346545A (en) | 2000-06-08 | 2001-12-18 | I Farm:Kk | Dietary supplement |
JP2002058451A (en) | 2000-08-21 | 2002-02-26 | Fancl Corp | Food composition |
JP2003201208A (en) | 2001-12-28 | 2003-07-18 | Ichimaru Pharcos Co Ltd | Cosmetic composition |
JP2008518042A (en) | 2004-10-07 | 2008-05-29 | アクセス ビジネス グループ インターナショナル エルエルシー | A composition comprising a rosemary (Rosmarinusofficinalis) plant extract, an Alpinia plant extract, and a DNA repair enzyme. |
JP2009242309A (en) | 2008-03-31 | 2009-10-22 | Ezaki Glico Co Ltd | Skin care preparation, oral composition, and food and drink |
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EP0904092B1 (en) * | 1996-05-18 | 2003-08-13 | Finzelberg GmbH & Co. KG | Purified extract of harpagophytum procumbens and/or harpagophytum zeyheri dence, process for its production and its use |
-
2019
- 2019-04-16 JP JP2020521782A patent/JP7461876B2/en active Active
- 2019-04-16 CN CN201980036121.2A patent/CN112203671A/en active Pending
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JP2001346545A (en) | 2000-06-08 | 2001-12-18 | I Farm:Kk | Dietary supplement |
JP2002058451A (en) | 2000-08-21 | 2002-02-26 | Fancl Corp | Food composition |
JP2003201208A (en) | 2001-12-28 | 2003-07-18 | Ichimaru Pharcos Co Ltd | Cosmetic composition |
JP2008518042A (en) | 2004-10-07 | 2008-05-29 | アクセス ビジネス グループ インターナショナル エルエルシー | A composition comprising a rosemary (Rosmarinusofficinalis) plant extract, an Alpinia plant extract, and a DNA repair enzyme. |
JP2009242309A (en) | 2008-03-31 | 2009-10-22 | Ezaki Glico Co Ltd | Skin care preparation, oral composition, and food and drink |
JP2016088929A (en) | 2014-10-30 | 2016-05-23 | 日光ケミカルズ株式会社 | Pollution preventing agent, and pollution preventing cosmetic or pollution preventing skin external preparation including the same |
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MNCWANGI NP et al.,What the devil is in your phytomedicine? Exploring species substitution in Harpagophytum through chemometric modeling of 1H-NMR and UHPLC-MS datasets,Phytochemistry,2014年,Vol.106,p.104-115,ISSN 0031-9422 |
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JPWO2019230233A1 (en) | 2021-06-10 |
CN112203671A (en) | 2021-01-08 |
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